Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth

被引：33

作者：

Qiao, LX

Zhao, LY

Rong, SB

Wu, XW

Wang, SM

Fujii, T

Kazanietz, MG

Rauser, L

Savage, J

Roth, BL

Flippen-Anderson, J

Kozikowski, AP ^{[1
]}

机构：

[1] Georgetown Univ, Ctr Med, Dept Neurol, Drug Discovery Program, Washington, DC 20007 USA

[2] Univ Penn, Sch Med, Ctr Expt Therapeut, Philadelphia, PA 19104 USA

[3] Case Western Reserve Univ, Dept Biochem & Neurosci, NIMH, Psychioact Drug Screening Program, Cleveland, OH 44106 USA

[4] USN, Res Lab, Washington, DC 20375 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(01)00097-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In view of its role in tumor promotion and signal transduction, protein kinase C (PKC) has proven to be an exciting target for cancer therapy. With the aid of molecular modeling, we rationally designed and stereoselectively synthesized a new class of rigidified pyrrolidone-based PKC activators. Pyrrolidone 15 was found to exhibit reasonable affinity for PKC delta, with lower affinity for the other isozymes tested. Pyrrolidone 2 causes the dose-dependent induction of apoptosis in LNCaP prostate cancer cells. This apoptotic effect could be markedly potentiated by the use of LNCaP cells overexpressing the PKC alpha or delta isozymes. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：955 / 959

页数：5

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