Inhibition of protein kinase C by dequalinium analogues: Structure-activity studies on head group variations

作     者：Abeywickrama, Chandima Rotenberg, Susan A. Baker, Arthur David 

作者机构：CUNY Grad Ctr Dept Chem New York NY 10016 USA CUNY Queens Coll Dept Chem & Biochem Flushing NY 11367 USA 

出 版 物：《BIOORGANIC & MEDICINAL CHEMISTRY》 (生物有机化学与医药化学)

年 卷 期：2006年第14卷第23期

页      面：7796-7803页

核心收录：

学科分类：0710[理学-生物学] 1007[医学-药学(可授医学、理学学位)] 071010[理学-生物化学与分子生物学] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 0703[理学-化学] 

基　　金：PSC-CUNY  (66380) 

主　　题：PKC inhibition head group role substituent effects quinolinium analogues 

摘      要：New dequalinium analogues and related heteroaromatic systems were synthesized and evaluated for inhibition of protein kinase Cot. In vitro assays with recombinant human PKC alpha showed that the number of the aromatic ring head groups as well as their electron-richness, are critical factors that determine potency. The inhibitory strengths of the synthesized compounds are shown to correlate well with Mulliken charges on the head group ring nitrogen atoms making it possible to design likely candidate molecules having improved protein kinase C alpha inhibitory activity. (c) 2006 Elsevier Ltd. All rights reserved.