Vascular endothelial growth factor receptor VEGFR inhibitors

Eskens FA et al (2006) The clinical toxicity profile of vascular endothelial growth factor (VEGF) and vascular endothelial growth factor receptor (VEGFR) targeting angiogenesis inhibitors a review. Eur J Cancer 42 3127-3139... 

Note of worth is also the successful replacement of the methyl ester with oxime ethers and Af-methoxy imidoyl nitrile in the design of muscarinic agonists (Figure 15.28). Several 1,2,4-oxadiazoles and the other five-mem-bered heterocycles are employed also for other therapeutic indications like monoamine transporter and opioid receptors,5-HT agonists, bradykinin Bi receptor antagonists, and vascular endothelial growth factor receptor (VEGFR-2) inhibitors. ... 

HT agonists, bradykinin Bi receptor antagonists,and vascular endothelial growth factor receptor (VEGFR-2) inhibitors. 

In addition to imatinib, some inhibitors of receptor tyrosine kinases targeting epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptors (VEGFR) and platelet-derived growth factor receptors (PDGFR) have been found to have antitumor and/or other activities. 

Pazopanib The effect of ketoconazole on the pharmacokinetics and safety of pazopanib, an oral tyrosine kinase inhibitor of vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2 and VEGFR-3), platelet-derived growth factor receptors (PDGFR-a and PDGFR-b) and c-kit was evaluated in 21 patients [59 ]. and AUC increased 42% and 40%, respectively. 

Optimization of the large (MW = 512), lipophilic (clogP = 7.6), and very potent (Kj = 0.22 nM) Vascular Endothelial Growth Factor Receptor Tyrosine Kinase (VEGFR TK) inhibitor 8 (LLE = 2.1) to produce the development candidate axitinib (9) was recently reported [17]. 

Compound 57 has been identified as a vascular endothelial growth factor receptor-2 (VEGFR-2) kinase inhibitor of interest for the treatment of cancer <20030PD676>. 

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