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设计和合成 3-(4,5,6,7-四氢-3H-咪唑并[4,5-c]吡啶-2-基)-1H-喹啉-2-酮作为 VEGFR-2 激酶抑制剂。

Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors.

机构信息

Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2837-42. doi: 10.1016/j.bmcl.2012.02.073. Epub 2012 Mar 7.

Abstract

A series of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones have been identified as a new class of VEGFR-2 kinase inhibitors. A variety of (4,5,6,7-tetrahydro-imidazo[5,4-c]pyridin-2-yl)-acetic acid ethyl esters were synthesized, and their VEGFR-2 inhibitory activity was evaluated. Described herein are the preparation of the series and the effects of the compounds on VEGFR-2 kinase activity.

摘要

一系列 3-(4,5,6,7-四氢-3H-咪唑并[4,5-c]吡啶-2-基)-1H-喹啉-2-酮已被鉴定为一类新的 VEGFR-2 激酶抑制剂。合成了多种(4,5,6,7-四氢-咪唑并[5,4-c]吡啶-2-基)-乙酸乙酯,并对其 VEGFR-2 抑制活性进行了评价。本文介绍了该系列化合物的制备及其对 VEGFR-2 激酶活性的影响。

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