个人信息Personal Information
教授
博士生导师
硕士生导师
性别:女
毕业院校:大连理工大学
学位:博士
所在单位:医学部
学科:化学生物学. 药理学. 细胞生物学
办公地点:Chemical complex building,D513
联系方式:zczhang@dlut.edu.cn 13942696903
电子邮箱:zczhang@dlut.edu.cn
Design, synthesis and structure-activity relationship studies of morpholino-1H-phenalene derivatives that antagonize Mcl-1/Bcl-2
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论文类型:期刊论文
发表时间:2014-11-01
发表刊物:BIOORGANIC & MEDICINAL CHEMISTRY
收录刊物:SCIE、PubMed、Scopus
卷号:22
期号:21
页面范围:5738-5746
ISSN号:0968-0896
关键字:Dual inhibitors; Hydrogen bond; Apoptosis; Mcl-1; Bcl-2
摘要:We report herein characteristic studies of Mcl-1 and Bcl-2 dual inhibitors. It was found that a protruding carbonyl group forming hydrogen bond with R263 plays a predominant role compared with the hydrophobic group that occupies the p2 pocket. A series of dual inhibitors representing different parts of the morpholino-1H-phenalene were designed, synthesized and evaluated. (C) 2014 Elsevier Ltd. All rights reserved.