[1]Kasak,Lagle;Näks,Mihkel;Eek,Priit;Piirsoo,Alla;Bhadoria,Rohit;Starkov,Pavel;Saarma,Merilin;Kasvandik,Sergo;Piirsoo,Marko[Biochemistry,2018,vol.57,#37,p.5456-5465]
Title: A phase I pharmacokinetic study of TSU-68 (a multiple tyrosine kinase inhibitor of VEGFR-2, FGF and PDFG) in combination with S-1 and oxaliplatin in metastatic colorectal cancer patients previously treated with chemotherapy.
Journal: Investigational new drugs 20120801
Title: The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Journal: Bioorganic & medicinal chemistry letters 20120801
Title: Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.
Journal: Bioorganic & medicinal chemistry 20120715
Title: N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.
Journal: Bioorganic & medicinal chemistry 20120401
Title: Augmentation of chemotherapeutic infusion effect by TSU-68, an oral targeted antiangiogenic agent, in a rabbit VX2 liver tumor model.
Journal: Cardiovascular and interventional radiology 20120201
Title: Phase I clinical study of the angiogenesis inhibitor TSU-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer.
Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120201
Title: Evaluation of molecular targeted cancer drug by changes in tumor marker doubling times.
Journal: Journal of gastroenterology 20120101
Title: Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.
Journal: Journal of medicinal chemistry 20110609
Title: Phase I, pharmacokinetic, and biological studies of TSU-68, a novel multiple receptor tyrosine kinase inhibitor, administered after meals with solid tumors.
Journal: Cancer chemotherapy and pharmacology 20110501
Title: Phase I and pharmacokinetic study of TSU-68, a novel multiple receptor tyrosine kinase inhibitor, by twice daily oral administration between meals in patients with advanced solid tumors.
Journal: Cancer chemotherapy and pharmacology 20110501
Title: A phase I/II trial of the oral antiangiogenic agent TSU-68 in patients with advanced hepatocellular carcinoma.
Journal: Cancer chemotherapy and pharmacology 20110201
Title: Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.
Journal: Bioorganic & medicinal chemistry 20100515
Title: 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.
Journal: Bioorganic & medicinal chemistry letters 20090201
Title: TSU68, an antiangiogenic receptor tyrosine kinase inhibitor, induces tumor vascular normalization in a human cancer xenograft nude mouse model.
Journal: Surgery today 20090101
Title: TSU68 prevents liver metastasis of colon cancer xenografts by modulating the premetastatic niche.
Journal: Cancer research 20081201
Title: Identification of human liver cytochrome P450 isoforms involved in autoinduced metabolism of the antiangiogenic agent (Z)-5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid (TSU-68).
Journal: Drug metabolism and disposition: the biological fate of chemicals 20080601
Title: Time-dependent induction of rat hepatic CYP1A1 and CYP1A2 expression after single-dose administration of the anti-angiogenic agent TSU-68.
Journal: Drug metabolism and pharmacokinetics 20080101
Title: The selectivity of protein kinase inhibitors: a further update.
Journal: The Biochemical journal 20071215
Title: Decrease in plasma concentrations of antiangiogenic agent TSU-68 ((Z)-5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid) during oral administration twice a day to rats.
Journal: Drug metabolism and disposition: the biological fate of chemicals 20070901
Title: Novel inhibitor for fibroblast growth factor receptor tyrosine kinase.
Journal: Bioorganic & medicinal chemistry letters 20070901
Title: Potent platelet-derived growth factor-beta receptor (PDGF-betaR) inhibitors: Synthesis and structure-activity relationships of 7-[3-(cyclohexylmethyl)ureido]-3-{1-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl}quinoxalin-2(1H)-one derivatives.
Journal: Chemical & pharmaceutical bulletin 20070201
Title: Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050901
Title: Inhibition of peritoneal dissemination of ovarian cancer by tyrosine kinase receptor inhibitor SU6668 (TSU-68).
Journal: International journal of cancer 20050320
Title: Vascular endothelial growth factor: a therapeutic target for tumors of the Ewing's sarcoma family.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050315
Title: Combined inhibition of vascular endothelial growth factor and platelet-derived growth factor signaling: effects on the angiogenesis, microcirculation, and growth of orthotopic malignant gliomas.
Journal: Journal of neurosurgery 20050201
Title: Combined antiangiogenic and immune therapy of prostate cancer.
Journal: Angiogenesis 20050101
Title: In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20040115
Title: Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.
Journal: Journal of medicinal chemistry 20030327
Title: Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.
Journal: Journal of medicinal chemistry 19991216
Title: Laird AD, et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res, 2000, 60(15), 4152-4160.
Title: Smolich BD, et al. The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts. Blood, 2001, 97(5), 1413-1421.
Title: Marzola P, et al. In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model. Clin Cancer Res, 2004, 10(2), 739-750.
Title: Kim HC, et al. Augmentation of chemotherapeutic infusion effect by TSU-68, an oral targeted antiangiogenic agent, in a rabbit VX2 liver tumor model. Cardiovasc Intervent Radiol. 2012 Feb;35(1):168-75
