2-substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity

被引：64

作者：

Kunick, C

Schultz, C

Lemcke, T

Zaharevitz, DW

Gussio, R

Jalluri, RK

Sausville, EA

Leost, M

Meijer, L

机构：

[1] Univ Hamburg, Inst Pharm, Abt Pharmazeut Chem, D-20146 Hamburg, Germany

[2] NCI, Dev Therapeut Program, Div Canc Treatment & Diag, Rockville, MD 20852 USA

[3] CNRS, Biol Stn, F-29682 Roscoff, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(00)00048-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

9-Trifluoromethyl-paullones with a carbon chain in the 2-position were synthesized by palladium-catalyzed coupling reactions of a 2-iodoprecursor with terminal alkenes or alkynes, respectively. The introduction of a 2-cyanoethyl substituent led to a significant enhancement of CDK1/cyclin B inhibiting property and in vitro antiproliferative activity. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：567 / 569

页数：3

共 15 条

[1] SOME PRACTICAL CONSIDERATIONS AND APPLICATIONS OF THE NATIONAL-CANCER-INSTITUTE IN-VITRO ANTICANCER DRUG DISCOVERY SCREEN [J].