In 2007,Kiselyov, Alexander S.; Milligan, Daniel; Ouyang, Xiaohu published 《Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates》.Bioorganic & Medicinal Chemistry Letters published the findings.Synthetic Route of C5H6N2O2 The information in the text is summarized as follows:
We have developed a series of novel potent 1-(2-(pyridin-4-yl)ethyl)-1H-azole-5-carboxamides active against kinases VEGFR-2 and -1. Both specific and dual ATP-competitive inhibitors of VEGFR-2 were identified. Kinase selectivity could be controlled by varying the 5-carboxamide substituent at the azole ring. The most specific mols. displayed >10-fold selectivity for VEGFR-2 over VEGFR-1. Compound activities in vitro and in cell-based assays (IC50 < 100 nM) were similar to those of reported clin. and development candidates, including PTK787 (Vatalanibtrade) and ZD6474 (Vandetanib). High permeability of active compounds across the Caco-2 cell monolayer (>40×10-5 cm/min) is indicative of their potential for intestinal absorption upon oral administration. In the part of experimental materials, we found many familiar compounds, such as Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Synthetic Route of C5H6N2O2)
Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Synthetic Route of C5H6N2O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics