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192185-72-1,MFCD07772347
Catalog No.:AA002FMA

192185-72-1 | Tipifarnib

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
98%
in stock  
$34.00   $24.00
- +
2mg
98%
in stock  
$57.00   $40.00
- +
5mg
98%
in stock  
$84.00   $59.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA002FMA
Chemical Name:
Tipifarnib
CAS Number:
192185-72-1
Molecular Formula:
C27H22Cl2N4O
Molecular Weight:
489.3958
MDL Number:
MFCD07772347
SMILES:
Clc1ccc(cc1)[C@](c1cncn1C)(c1ccc2c(c1)c(cc(=O)n2C)c1cccc(c1)Cl)N
Properties
Properties
 
BP:
681.7°C at 760 mmHg  
Form:
Solid  
MP:
211-213°C (dec.)  
Storage:
Inert atmosphere;-20 ℃;  

Computed Properties
 
Complexity:
785  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
34  
Hydrogen Bond Acceptor Count:
3  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
4  
XLogP3:
4.1  

Downstream Synthesis Route

[1]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

CASUnavailable 
  192185-72-1 

[1]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[2]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[1]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[2]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[3]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[4]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

7497-60-1   
tipifarnib 

[1]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[2]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[3]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[4]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[1]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[2]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[3]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

[4]Angibaud,PatrickR.;Venet,MarcG.;Filliers,Walter;Broeckx,Rudy;Ligny,YannickA.;Muller,Philippe;Poncelet,VirginieS.;End,DaveW.[EuropeanJournalofOrganicChemistry,2004,#3,p.479-486]

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Title: Managing myelodysplastic symptoms in elderly patients.

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Title: Targeted therapy in the treatment of malignant gliomas.

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Title: Phase I trial of tipifarnib in children with newly diagnosed intrinsic diffuse brainstem glioma.

Journal: Neuro-oncology 20080601

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Title: Phase II trial of tipifarnib as maintenance therapy in first complete remission in adults with acute myelogenous leukemia and poor-risk features.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080515

Title: Farnesyltransferase inhibitors and their potential role in therapy for myelodysplastic syndromes and acute myeloid leukaemia.

Journal: British journal of haematology 20080501

Title: Medullary thyroid cancer: targeting the RET kinase pathway with sorafenib/tipifarnib.

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Title: Farnesyltransferase inhibitor R115777 inhibits cell growth and induces apoptosis in mantle cell lymphoma.

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Title: Phase I study of alternate-week administration of tipifarnib in patients with myelodysplastic syndrome.

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Title: In vitro effects of the farnesyltransferase inhibitor tipifarnib on myelodysplastic syndrome progenitors.

Journal: Acta haematologica 20080101

Title: A phase II study of the farnesyl transferase inhibitor, tipifarnib, in children with recurrent or progressive high-grade glioma, medulloblastoma/primitive neuroectodermal tumor, or brainstem glioma: a Children's Oncology Group study.

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Title: Small-molecule and antibody approaches to molecular chemotherapy of primary brain tumors.

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Title: Gateways to clinical trials.

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Title: The RAS/mitogen activated protein (MAP) kinase pathway in melanoma biology and therapeutics.

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Title: Tipifarnib in the treatment of acute myeloid leukemia.

Journal: Biologics : targets & therapy 20071201

Title: The farnesyltransferase inhibitor R115777 (ZARNESTRA) enhances the pro-apoptotic activity of interferon-alpha through the inhibition of multiple survival pathways.

Journal: International journal of cancer 20071115

Title: Novel therapeutic strategies combining antihormonal and biological targeted therapies in breast cancer: focus on clinical trials and perspectives.

Journal: Critical reviews in oncology/hematology 20071101

Title: Phase 1 study of tipifarnib in combination with imatinib for patients with chronic myelogenous leukemia in chronic phase after imatinib failure.

Journal: Cancer 20071101

Title: Tipifarnib in acute myeloid leukemia.

Journal: Drugs of today (Barcelona, Spain : 1998) 20071101

Title: Femara and the future: tailoring treatment and combination therapies with Femara.

Journal: Breast cancer research and treatment 20071001

Title: Decitabine in the treatment of myelodysplastic syndromes.

Journal: Therapeutics and clinical risk management 20071001

Title: Farnesyltransferase inhibitors inhibit T-cell cytokine production at the posttranscriptional level.

Journal: Blood 20070915

Title: A phase II trial of tipifarnib in myelofibrosis: primary, post-polycythemia vera and post-essential thrombocythemia.

Journal: Leukemia 20070901

Title: Cloning and characterization of a human BCR/ABL-positive cell line, K562/RR, resistant to the farnesyltransferase inhibition by tipifarnib.

Journal: Experimental hematology 20070901

Title: The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo.

Journal: Molecular cancer therapeutics 20070901

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20070901

Title: On the diversity of biological therapeutics.

Journal: Biologics : targets & therapy 20070901

Title: The molecular genetics of breast cancer and targeted therapy.

Journal: Biologics : targets & therapy 20070901

Title: Exposure-toxicity relationships for tipifarnib in cancer patients.

Journal: British journal of clinical pharmacology 20070801

Title: Phase I trial of tipifarnib (R115777) concurrent with radiotherapy in patients with glioblastoma multiforme.

Journal: International journal of radiation oncology, biology, physics 20070801

Title: Exploiting signal transduction pathways in acute myelogenous leukemia.

Journal: Current treatment options in oncology 20070801

Title: Farnesyltransferase inihibitors in hematologic malignancies.

Journal: Blood reviews 20070701

Title: A phase 2 study of the oral farnesyltransferase inhibitor tipifarnib in patients with refractory or relapsed acute myeloid leukemia.

Journal: Blood 20070615

Title: A multicenter phase 2 study of the farnesyltransferase inhibitor tipifarnib in intermediate- to high-risk myelodysplastic syndrome.

Journal: Blood 20070515

Title: The farnesyltransferase inhibitor R115777 up-regulates the expression of death receptor 5 and enhances TRAIL-induced apoptosis in human lung cancer cells.

Journal: Cancer research 20070515

Title: A preclinical evaluation of pemetrexed and irinotecan combination as second-line chemotherapy in pancreatic cancer.

Journal: British journal of cancer 20070507

Title: R115777 (Zarnestra)/Zoledronic acid (Zometa) cooperation on inhibition of prostate cancer proliferation is paralleled by Erk/Akt inactivation and reduced Bcl-2 and bad phosphorylation.

Journal: Journal of cellular physiology 20070501

Title: Impact on farnesyltransferase inhibition of 4-chlorophenyl moiety replacement in the Zarnestra series.

Journal: European journal of medicinal chemistry 20070501

Title: The incidence and impact of thrombocytopenia in myelodysplastic syndromes.

Journal: Cancer 20070501

Title: A phase I clinical and pharmacokinetic study of tipifarnib in combination with docetaxel in patients with advanced solid malignancies.

Journal: Current medical research and opinion 20070501

Title: Massive plexiform neurofibromas in childhood: natural history and management issues.

Journal: Journal of neurosurgery 20070501

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20070501

Title: The farnesyl transferase inhibitor, tipifarnib, is a potent inhibitor of the MDR1 gene product, P-glycoprotein, and demonstrates significant cytotoxic synergism against human leukemia cell lines.

Journal: Leukemia 20070401

Title: Diseases of large granular lymphocytes.

Journal: Cancer control : journal of the Moffitt Cancer Center 20070401

Title: Identification of molecular predictors of response in a study of tipifarnib treatment in relapsed and refractory acute myelogenous leukemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070401

Title: Oncogenic K-Ras signals through epidermal growth factor receptor and wild-type H-Ras to promote radiation survival in pancreatic and colorectal carcinoma cells.

Journal: Neoplasia (New York, N.Y.) 20070401

Title: Clinical activity of tipifarnib in hematologic malignancies.

Journal: Expert opinion on investigational drugs 20070301

Title: The emerging role of targeted therapy for hematologic malignancies: update on bortezomib and tipifarnib.

Journal: The oncologist 20070301

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20070301

Title: A phase 2 study of the farnesyltransferase inhibitor tipifarnib in poor-risk and elderly patients with previously untreated acute myelogenous leukemia.

Journal: Blood 20070215

Title: [Prognostic molecular marker and molecular targeted-therapy in pediatric malignancies].

Journal: Gan to kagaku ryoho. Cancer & chemotherapy 20070201

Title: Prevention of mouse lung tumors and modulation of DNA methylation by combined treatment with budesonide and R115777 (Zarnestra MT).

Journal: Carcinogenesis 20070101

Title: 48th annual meeting of the American Society of Hematology December 9-12, 2006, Orlando, FL.

Journal: Clinical lymphoma & myeloma 20070101

Title: E2902: A Phase III randomized study of farnesyl transferase inhibitor R115777 in acute myeloid leukemia patients in second or subsequent remission or in remission after primary induction failure or patients over age 60 in first remission.

Journal: Clinical advances in hematology & oncology : H&O 20070101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20070101

Title: Clinical trials update: endocrine and biological therapy combinations in the treatment of breast cancer.

Journal: Breast cancer research : BCR 20070101

Title: Suicide candidate genes associated with bipolar disorder and schizophrenia: an exploratory gene expression profiling analysis of post-mortem prefrontal cortex.

Journal: BMC genomics 20070101

Title: New and old treatment modalities in primary myelofibrosis.

Journal: Cancer journal (Sudbury, Mass.) 20070101

Title: Prevention of mouse lung tumors and modulation of DNA methylation by combined treatment with budesonide and R115777 (ZarnestraMT).

Journal: Carcinogenesis 20061201

Title: Azacytidine (Vidaza(R)) in the treatment of myelodysplastic syndromes.

Journal: Therapeutics and clinical risk management 20061201

Title: Role of erlotinib in the management of pancreatic cancer.

Journal: Therapeutics and clinical risk management 20061201

Title: Effect of CYP2D6 genetic polymorphism on the population pharmacokinetics of tipifarnib.

Journal: Cancer chemotherapy and pharmacology 20061101

Title: A phase I safety, pharmacological and biological study of the farnesyl protein transferase inhibitor, tipifarnib and capecitabine in advanced solid tumors.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20061101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20061101

Title: Depletion of substrates for protein prenylation increases apoptosis in human periovulatory granulosa cells.

Journal: Molecular reproduction and development 20061001

Title: Pharmacokinetics of tipifarnib after oral and intravenous administration in subjects with advanced cancer.

Journal: Journal of clinical pharmacology 20061001

Title: Clinical and pharmacologic study of the farnesyltransferase inhibitor tipifarnib in cancer patients with normal or mildly or moderately impaired hepatic function.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20061001

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20061001

Title: Combination therapy with aromatase inhibitors: the next era of breast cancer treatment?

Journal: British journal of cancer 20060918

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20060901

Title: Phase II trial of tipifarnib in patients with recurrent malignant glioma either receiving or not receiving enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060801

Title: Efficacy of the farnesyltransferase inhibitor R115777 in a rat mammary tumor model: role of Ha-ras mutations and use of microarray analysis in identifying potential targets.

Journal: Carcinogenesis 20060701

Title: Phase II trial of R115777 (NSC #70818) in patients with advanced colorectal cancer: a Southwest Oncology Group study.

Journal: Investigational new drugs 20060701

Title: Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060701

Title: HDJ-2 as a target for radiosensitization of glioblastoma multiforme cells by the farnesyltransferase inhibitor R115777 and the role of the p53/p21 pathway.

Journal: Cancer research 20060701

Title: Population pharmacokinetics of tipifarnib in healthy subjects and adult cancer patients.

Journal: British journal of clinical pharmacology 20060701

Title: Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials.

Journal: British journal of cancer 20060424

Title: Anti-inflammatory activity in vitro and in vivo of the protein farnesyltransferase inhibitor tipifarnib.

Journal: The Journal of pharmacology and experimental therapeutics 20060401

Title: [Farnesyl transferase inhibitors--a novel agent for breast cancer].

Journal: Ai zheng = Aizheng = Chinese journal of cancer 20060401

Title: Effects of the farnesyl transferase inhibitor R115777 (Zarnestra) on mammary carcinogenesis: prevention, therapy, and role of HaRas mutations.

Journal: Molecular cancer therapeutics 20060401

Title: [Molecular targets in colon cancer].

Journal: Therapeutische Umschau. Revue therapeutique 20060401

Title: Raltitrexed-eloxatin salvage chemotherapy in gemcitabine-resistant metastatic pancreatic cancer.

Journal: British journal of cancer 20060327

Title: Tipifarnib: farnesyl transferase inhibition at a crossroads.

Journal: Expert review of anticancer therapy 20060301

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20060301

Title: Farnesyltransferase inhibitors in myelodysplastic syndrome.

Journal: Current hematologic malignancy reports 20060301

Title: Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060120

Title: Tipifarnib and bortezomib are synergistic and overcome cell adhesion-mediated drug resistance in multiple myeloma and acute myeloid leukemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20060115

Title: Non-transplant therapy for older adults with acute myeloid leukemia.

Journal: Journal of the National Comprehensive Cancer Network : JNCCN 20060101

Title: Myelodysplasia: when to treat and how.

Journal: Best practice & research. Clinical haematology 20060101

Title: Effect of a farnesyl transferase inhibitor (R115777) on ductal carcinoma in situ of the breast in a human xenograft model and on breast and ovarian cancer cell growth in vitro and in vivo.

Journal: Breast cancer research : BCR 20060101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20051201

Title: Development of the farnesyltransferase inhibitor tipifarnib for therapy of hematologic malignancies.

Journal: Future oncology (London, England) 20051201

Title: Phase I and pharmacological study of the farnesyltransferase inhibitor tipifarnib (Zarnestra, R115777) in combination with gemcitabine and cisplatin in patients with advanced solid tumours.

Journal: British journal of cancer 20051128

Title: In vitro profiling of the sensitivity of pediatric leukemia cells to tipifarnib: identification of T-cell ALL and FAB M5 AML as the most sensitive subsets.

Journal: Blood 20051115

Title: Nitrogen-containing bisphosphonate incadronate augments the inhibitory effect of farnesyl transferase inhibitor tipifarnib on the growth of fresh and cloned myeloma cells in vitro.

Journal: Leukemia & lymphoma 20051101

Title: Farnesyl transferase inhibition in hematologic malignancies.

Journal: Journal of the National Comprehensive Cancer Network : JNCCN 20051101

Title: A phase II study of farnesyl transferase inhibitor R115777 in pancreatic cancer: a Southwest oncology group (SWOG 9924) study.

Journal: Investigational new drugs 20051001

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20051001

Title: Phase I trial of tipifarnib in patients with recurrent malignant glioma taking enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050920

Title: Docetaxel induces p53-dependent apoptosis and synergizes with farnesyl transferase inhibitor r115777 in human epithelial cancer cells.

Journal: Frontiers in bioscience : a journal and virtual library 20050901

Title: Development of farnesyl transferase inhibitors: a review.

Journal: The oncologist 20050901

Title: The protein farnesyltransferase inhibitor Tipifarnib as a new lead for the development of drugs against Chagas disease.

Journal: Journal of medicinal chemistry 20050825

Title: Characterization of a R115777-resistant human multiple myeloma cell line with cross-resistance to PS-341.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050815

Title: Conventional and new treatment options for myelofibrosis with myeloid metaplasia.

Journal: Seminars in oncology 20050801

Title: Farnesyltransferase inhibitor R115777 (Zarnestra, Tipifarnib) synergizes with paclitaxel to induce apoptosis and mitotic arrest and to inhibit tumor growth of multiple myeloma cells.

Journal: Blood 20050615

Title: Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.

Journal: Bioorganic & medicinal chemistry letters 20050602

Title: Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.

Journal: Journal of medicinal chemistry 20050602

Title: Relative importance of apoptosis and cell cycle blockage in the synergistic effect of combined R115777 and imatinib treatment in BCR/ABL-positive cell lines.

Journal: Biochemical pharmacology 20050601

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20050601

Title: A phase II trial of R115777, an oral farnesyl transferase inhibitor, in patients with advanced urothelial tract transitional cell carcinoma.

Journal: Cancer 20050515

Title: Farnesyltransferase inhibitor tipifarnib (R115777) preferentially inhibits in vitro autonomous erythropoiesis of polycythemia vera patient cells.

Journal: Blood 20050501

Title: Isoprenylation of intracellular proteins as a new target for the therapy of human neoplasms: preclinical and clinical implications.

Journal: Current drug targets 20050501

Title: Farnesyltransferase inhibitors in myelodysplastic syndrome.

Journal: Current hematology reports 20050501

Title: Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20050415

Title: Farnesyl transferase inhibitor (R115777)-induced inhibition of STAT3(Tyr705) phosphorylation in human pancreatic cancer cell lines require extracellular signal-regulated kinases.

Journal: Cancer research 20050401

Title: In vivo apoptosis detection with radioiodinated Annexin V in LoVo tumour-bearing mice following Tipifarnib (Zarnestra, R115777) farnesyltransferase inhibitor therapy.

Journal: Nuclear medicine and biology 20050401

Title: Current and future perspectives on fulvestrant.

Journal: Clinical breast cancer 20050401

Title: Molecule of the month. Tipifarnib.

Journal: Drug news & perspectives 20050401

Title: Intermittent dosing of the farnesyl transferase inhibitor tipifarnib (R115777) in advanced malignant solid tumors: a phase I California Cancer Consortium Trial.

Journal: Anti-cancer drugs 20050301

Title: [Farnesyltransferase inhibitors: preliminary results in acute myeloid leukemia].

Journal: Bulletin du cancer 20050301

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20050301

Title: Farnesyltransferase inhibitors.

Journal: Clinical advances in hematology & oncology : H&O 20050301

Title: [New targets for molecular therapy of acute leukemia: a 'single-hit' or 'multiple-hit' strategy against signaling pathway].

Journal: Zhonghua yi xue za zhi 20050223

Title: Synthesis, biodistribution and effects of farnesyltransferase inhibitor therapy on tumour uptake in mice of 99mTc labelled epidermal growth factor.

Journal: Nuclear medicine communications 20050201

Title: A phase I trial and pharmacokinetic study of tipifarnib, a farnesyltransferase inhibitor, and tamoxifen in metastatic breast cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050201

Title: Farnesyltransferase inhibitor therapy in acute myelogenous leukemia.

Journal: Current hematology reports 20050101

Title: The American Society of Hematology--46th Annual Meeting and Exposition. HDAC, Flt and farnesyl transferase inhibitors.

Journal: IDrugs : the investigational drugs journal 20050101

Title: New agents in intravesical chemotherapy of superficial bladder cancer.

Journal: Scandinavian journal of urology and nephrology 20050101

Title: Biomarkers of anticancer activity of R115777 (Tipifarnib, Zarnestra) in human breast cancer models in vitro.

Journal: Anticancer research 20050101

Title: Farnesyltransferase inhibitors.

Journal: Cancer chemotherapy and biological response modifiers 20050101

Title: New concepts in the treatment of acute myeloid malignancies: selected pathways for targeted therapy.

Journal: Journal of biological regulators and homeostatic agents 20050101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20050101

Title: Farnesyl-transferase inhibitor R115,777 enhances tamoxifen inhibition of MCF-7 cell growth through estrogen receptor dependent and independent pathways.

Journal: Breast cancer research : BCR 20050101

Title: [Problems in the current target therapy of malignancies].

Journal: Voprosy onkologii 20050101

Title: The influence of farnesyl protein transferase inhibitor R115777 (Zarnestra) alone and in combination with purine nucleoside analogs on acute myeloid leukemia progenitors in vitro.

Journal: European journal of haematology 20041201

Title: Dose-ranging pharmacodynamic study of tipifarnib (R115777) in patients with relapsed and refractory hematologic malignancies.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20041201

Title: Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20041101

Title: Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20041101

Title: Clinical activity of farnesyl transferase inhibitors in hematologic malignancies: possible mechanisms of action.

Journal: Leukemia & lymphoma 20041101

Title: [Multiple myeloma: from molecular pathogenensis to the development of molecular targeting therapies].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology 20041101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20041101

Title: Phase III double-blind placebo-controlled study of farnesyl transferase inhibitor R115777 in patients with refractory advanced colorectal cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20041001

Title: The farnesyl transferase inhibitor R115777 (Zarnestra) synergistically enhances growth inhibition and apoptosis induced on epidermoid cancer cells by Zoledronic acid (Zometa) and Pamidronate.

Journal: Oncogene 20040909

Title: Investigation of the effect of the farnesyl protein transferase inhibitor R115777 on isoprenylation and intracellular signalling by the prostacyclin receptor.

Journal: British journal of pharmacology 20040901

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20040901

Title: Quantile estimation following non-parametric phase I clinical trials with ordinal response.

Journal: Statistics in medicine 20040830

Title: Pharmacogenetics of tipifarnib (R115777) transport and metabolism in cancer patients.

Journal: Investigational new drugs 20040801

Title: Influence of farnesyl transferase inhibitor treatment on epidermal growth factor receptor status.

Journal: Nuclear medicine and biology 20040801

Title: Phase II study of the farnesyl transferase inhibitor R115777 in patients with sensitive relapse small-cell lung cancer.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20040801

Title: Studies of the isoprenoid-mediated inhibition of mevalonate synthesis applied to cancer chemotherapy and chemoprevention.

Journal: Experimental biology and medicine (Maywood, N.J.) 20040701

Title: Farnesyltransferase inhibitors as anticancer agents: critical crossroads.

Journal: Current opinion in drug discovery & development 20040701

Title: Farnesyl transferase inhibitors for patients with lung cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20040615

Title: Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity.

Journal: Biochemistry 20040608

Title: Phase I and pharmacokinetic study of the farnesyltransferase inhibitor R115777 in combination with irinotecan in patients with advanced cancer.

Journal: Cancer chemotherapy and pharmacology 20040601

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20040601

Title: Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma.

Journal: Blood 20040501

Title: Farnesyl transferase inhibitor R115777 in myelodysplastic syndrome.

Journal: Current hematology reports 20040501

Title: Phase I and pharmacokinetic study of irinotecan in combination with R115777, a farnesyl protein transferase inhibitor.

Journal: British journal of cancer 20040419

Title: Phase III trial of gemcitabine plus tipifarnib compared with gemcitabine plus placebo in advanced pancreatic cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20040415

Title: Phase II study of R115777, a farnesyl transferase inhibitor, in myelodysplastic syndrome.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20040401

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20040401

Title: Targeted therapies in myelodysplastic syndromes: ASH 2003 review.

Journal: Seminars in hematology 20040401

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20040301

Title: R115777 induces Ras-independent apoptosis of myeloma cells via multiple intrinsic pathways.

Journal: Molecular cancer therapeutics 20040201

Title: Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.

Journal: Journal of medicinal chemistry 20040129

Title: [Molecular pathogenesis of chronic myeloid leukemia and tyrosine kinase inhibitor].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology 20040101

Title: Microarray analysis reveals genetic pathways modulated by tipifarnib in acute myeloid leukemia.

Journal: BMC cancer 20040101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20040101

Title: New targets for therapy in breast cancer: farnesyltransferase inhibitors.

Journal: Breast cancer research : BCR 20040101

Title: [Ras signaling pathway as a target for farnesyltransferase inhibitors--a new, promising prospects in the treatment for malignant disorders].

Journal: Wiadomosci lekarskie (Warsaw, Poland : 1960) 20040101

Title: Farnesyltransferase inhibitor R115777 in myelodysplastic syndrome: clinical and biologic activities in the phase 1 setting.

Journal: Blood 20031215

Title: 4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.

Journal: Bioorganic & medicinal chemistry letters 20031215

Title: Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20031215

Title: The farnesyltransferase inhibitor R115777 reduces hypoxia and matrix metalloproteinase 2 expression in human glioma xenograft.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20031201

Title: Effect of farnesyl transferase inhibitor R115777 on the growth of fresh and cloned myeloma cells in vitro.

Journal: Blood 20031101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20031101

Title: A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20031015

Title: Molecular neuro-oncology and development of targeted therapeutic strategies for brain tumors. Part 1: Growth factor and Ras signaling pathways.

Journal: Expert review of anticancer therapy 20031001

Title: Farnesyltransferase inhibitors and their potential in the treatment of breast carcinoma.

Journal: Seminars in oncology 20031001

Title: Farnesyl transferase inhibitors in myeloid malignancies.

Journal: Blood reviews 20030901

Title: Effects of the farnesyl transferase inhibitor R115777 on normal and leukemic hematopoiesis.

Journal: Leukemia 20030901

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20030901

Title: Primary and secondary prevention of non-small-cell lung cancer: the SPORE Trials of Lung Cancer Prevention.

Journal: Clinical lung cancer 20030901

Title: Farnesyltransferase inhibitors in acute myeloid leukemia and myelodysplastic syndromes.

Journal: Clinical lymphoma 20030801

Title: New drugs in acute myeloid leukemia.

Journal: Clinical advances in hematology & oncology : H&O 20030801

Title: Phase II study of the efficacy and tolerability of two dosing regimens of the farnesyl transferase inhibitor, R115777, in advanced breast cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20030701

Title: A Phase I trial of the farnesyl protein transferase inhibitor R115777 in combination with gemcitabine and cisplatin in patients with advanced cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20030701

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20030601

Title: 5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20030505

Title: Phase II study of the farnesyl transferase inhibitor R115777 in patients with advanced non-small-cell lung cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20030501

Title: Chemoprevention of benzo(a)pyrene-induced lung tumors in mice by the farnesyltransferase inhibitor R115777.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20030501

Title: In vitro antiproliferative activity of the farnesyltransferase inhibitor R115777 in hematopoietic progenitors from patients with myelofibrosis with myeloid metaplasia.

Journal: Leukemia 20030501

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20030501

Title: Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.

Journal: Bioorganic & medicinal chemistry letters 20030407

Title: Phase II and pharmacodynamic study of the farnesyltransferase inhibitor R115777 as initial therapy in patients with metastatic pancreatic adenocarcinoma.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20030401

Title: Efficacy of the farnesyl transferase inhibitor R115777 in chronic myeloid leukemia and other hematologic malignancies.

Journal: Blood 20030301

Title: Preclinical and clinical evaluation of farnesyltransferase inhibitors.

Journal: Current oncology reports 20030301

Title: Farnesyl transferase inhibitors in the treatment of breast cancer.

Journal: Expert opinion on investigational drugs 20030301

Title: Inhibiting Ras signaling in the therapy of breast cancer.

Journal: Clinical breast cancer 20030201

Title: Molecular targeting therapy for cancer: the Twelfth International Symposium of the Hiroshima Cancer Seminar, November 2002.

Journal: Cancer science 20030201

Title: Targeting RAS signalling pathways in cancer therapy.

Journal: Nature reviews. Cancer 20030101

Title: The prolyl isomerase Pin1 in breast development and cancer.

Journal: Breast cancer research : BCR 20030101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20030101

Title: Farnesyl protein transferase inhibitor ZARNESTRA R115777 - history of a discovery.

Journal: Current topics in medicinal chemistry 20030101

Title: Farnesyltransferase inhibitors--a novel approach in the treatment of advanced pancreatic carcinomas.

Journal: Anticancer research 20030101

Title: Clinical research in pancreatic cancer: the Radiation Therapy Oncology Group trials.

Journal: International journal of radiation oncology, biology, physics 20030101

Title: Gemcitabine in the treatment of advanced pancreatic cancer: a comparative analysis of randomized trials.

Journal: Seminars in oncology 20021201

Title: [Innovative treatment in oncology].

Journal: Recenti progressi in medicina 20021101

Title: [New data presented at ASCO 2002 concerning small cell bronchial cancer].

Journal: Revue de pneumologie clinique 20021101

Title: Farnesyl transferase inhibitors as anticancer agents.

Journal: European journal of cancer (Oxford, England : 1990) 20020901

Title: Farnesyl transferase inhibitor R115777 induces apoptosis of human myeloma cells.

Journal: Leukemia 20020901

Title: Farnesyl transferase inhibitors: a major breakthrough in anticancer therapy? Naples, 12 April 2002.

Journal: Anti-cancer drugs 20020901

Title: Gateways to Clinical Trials.

Journal: Methods and findings in experimental and clinical pharmacology 20020901

Title: [New therapeutic targets and strategies in lung cancer].

Journal: Archivos de bronconeumologia 20020801

Title: Evaluation of accelerator mass spectrometry in a human mass balance and pharmacokinetic study-experience with 14C-labeled (R)-6-[amino(4- chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1- methyl-2(1H)-quinolinone (R115777), a farnesyl transferase inhibitor.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20020701

Title: Farnesyltransferase inhibitor, R115777, reverses the resistance of human glioma cell lines to ionizing radiation.

Journal: International journal of cancer 20020701

Title: Clinical trials referral resource. Current clinical trials of R115777 (Zarnestra).

Journal: Oncology (Williston Park, N.Y.) 20020701

Title: Phase I clinical and pharmacologic study of chronic oral administration of the farnesyl protein transferase inhibitor R115777 in advanced cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20020601

Title: Establishment and characterization of acquired resistance to the farnesyl protein transferase inhibitor R115777 in a human colon cancer cell line.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20020601

Title: Synergism of aminobisphosphonates and farnesyl transferase inhibitors on tumor metastasis.

Journal: Clinical orthopaedics and related research 20020401

Title: Tipifarnib (Janssen Pharmaceutica).

Journal: Current opinion in investigational drugs (London, England : 2000) 20020201

Title: Evaluation of the bioequivalence of tablets and capsules containing the novel anticancer agent R115777 (Zarnestra) in patients with advanced solid tumors.

Journal: European journal of drug metabolism and pharmacokinetics 20020101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20020101

Title: Agents targeting ras signaling pathway.

Journal: Current pharmaceutical design 20020101

Title: Farnesyltransferase inhibitors in breast cancer therapy.

Journal: Cancer investigation 20020101

Title: Current status of clinical trials of farnesyltransferase inhibitors.

Journal: Current opinion in oncology 20011101

Title: Preclinical antitumor activity and pharmacodynamic studies with the farnesyl protein transferase inhibitor R115777 in human breast cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20011101

Title: Farnesyltransferase inhibitors.

Journal: Seminars in oncology 20011001

Title: Cancer therapy. New strategies and treatment modalities for optimizing patient outcomes.

Journal: Seminars in hematology 20010701

Title: Farnesyl protein transferase inhibitors as targeted therapies for hematologic malignancies.

Journal: Seminars in hematology 20010701

Title: Clinical and biologic activity of the farnesyltransferase inhibitor R115777 in adults with refractory and relapsed acute leukemias: a phase 1 clinical-laboratory correlative trial.

Journal: Blood 20010601

Title: Magnetic resonance detects changes in phosphocholine associated with Ras activation and inhibition in NIH 3T3 cells.

Journal: British journal of cancer 20010301

Title: Phase I and pharmacokinetic study of the orally administered farnesyl transferase inhibitor R115777 in patients with advanced solid tumors.

Journal: Anti-cancer drugs 20010301

Title: Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.

Journal: Cancer research 20010101

Title: Farnesylated proteins and cell cycle progression.

Journal: Journal of cellular biochemistry. Supplement 20010101

Title: Devendra S Puntambekar, et al. Inhibition of farnesyltransferase: a rational approach to treat cancer? J Enzyme Inhib Med Chem. 2007 Apr;22(2):127-40.

Title: Martin LA, et al. The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with ICI 47699 acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo. Mol Cancer Ther. 2007 Sep;6(9):2

Title: End DW, et al. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 2001 Jan 1;61(1):131-7

Title: Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161.

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