Novel, potent and selective cyclin D1/CDK4 inhibitors:: Indolo[6,7-a]pyrrolo[3,4-c]carbazoles

被引：57

作者：

Engler, TA ^{[1
]}

Furness, K

Malhotra, S

Sanchez-Martinez, C

Shih, C

Xie, W

Zhu, GX

Zhou, X

Conner, S

Faul, MM

Sullivan, KA

Kolis, SP

Brooks, HB

Patel, B

Schultz, RM

DeHahn, TB

Kirmani, K

Spencer, CD

Watkins, SA

Considine, EL

Dempsey, JA

Ogg, CA

Stamm, NB

Anderson, BD

Campbell, RM

Vasudevan, V

Lytle, ML

机构：

[1] Eli Lilly & Co, Lilly Res Lab, Indianapolis, IN 46285 USA

[2] Lilly Spain SA, Madrid 28108, Spain

[3] Eli Lilly & Co, Chem Proc Res & Dev, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(03)00461-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：2261 / 2267

页数：7

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