Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening

被引：47

作者：

Usui, Taikou ^{[1
]}

Ban, Hyun Seung ^{[1
]}

Kawada, Junpei ^{[1
]}

Hirokawa, Takatsugu ^{[2
]}

Nakamura, Hiroyuki ^{[1
]}

机构：

[1] Gakushuin Univ, Fac Sci, Dept Chem, Tokyo 1718588, Japan

[2] Inst Adv Ind Sci & Technol AIST, Computat Biol Res Ctr, Tokyo 1350064, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

D O I：

10.1016/j.bmcl.2007.10.084

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of indenopyrazoles 8 and 9 were designed and synthesized as EGFR tyrosine kinase inhibitors by in silico high-throughput screening. Compounds 8b and 8d showed significant inhibition of A431 cell growth (GI(50) = 0.062 and 0.057 mu M, respectively). Compounds 8b and 9a showed inhibitory activity toward both EGFR and VEGFR-2 (KDR) tyrosine kinases, whereas 8d inhibited VEGFR-2 tyrosine kinase, exclusively. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：285 / 288

页数：4

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