Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors

被引：39

作者：

Zhu, GX ^{[1
]}

Conner, S ^{[1
]}

Zhou, X ^{[1
]}

Shih, C ^{[1
]}

Brooks, HB ^{[1
]}

Considine, E ^{[1
]}

Dempsey, JA ^{[1
]}

Ogg, C ^{[1
]}

Patel, B ^{[1
]}

Schultz, RM ^{[1
]}

Spencer, CD ^{[1
]}

Teicher, B ^{[1
]}

Watkins, SA ^{[1
]}

机构：

[1] Eli Lilly & Co, Lilly Corp Ctr, Lilly Res Labs, A Div, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(03)00133-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of pyrrolo[3,4-c] carbazoles fused with a quinolinyl/isoquinolinyl moiety were synthesized and their D1/CDK4 inhibitory and antiproliferative activity were evaluated. Compound 8H, 14H-isoquinolinyl[6,5-a]-pyrrolo[3,4-c]carbazole-7,9-dione (1d) was found to be a highly potent D1/CDK4 inhibitor with an IC50 of 69 nM. Compound Id also inhibited tumor cell growth, arrested tumor cells in G1 phase and inhibited pRb phosphorylation. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1231 / 1235

页数：5

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