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

…, HS Ban, J Kawada, T Hirokawa, H Nakamura

Index: Usui, Taikou; Ban, Hyun Seung; Kawada, Junpei; Hirokawa, Takatsugu; Nakamura, Hiroyuki Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 285 - 288

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Citation Number: 22

Abstract

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 (GI50= 0.062 and 0.057 μM, 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.