张志超

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

扫描关注

论文成果

当前位置: 中文主页 >> 科学研究 >> 论文成果

Design, synthesis and structure-activity relationship studies of morpholino-1H-phenalene derivatives that antagonize Mcl-1/Bcl-2

点击次数:

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.