Mono-carbonyl curcumin analogues as 11β-hydroxysteroid dehydrogenase 1 inhibitors

被引：11
|
作者：
Lin, Han [1 ,2 ,4 ]
Hu, Guo-Xin [1 ,2 ,3 ]
Guo, Jingjing [1 ,2 ]
Ge, Yufei [4 ,5 ]
Liang, Guang [3 ]
Lian, Qing-Quan [1 ,2 ]
Chu, Yanhui
Yuan, Xiaohuan
Huang, Ping [6 ]
Ge, Ren-Shan [1 ,2 ]
机构：
[1] Wenzhou Med Coll, Affiliated Hosp 2, Wenzhou 325000, Peoples R China
[2] Wenzhou Med Coll, Inst Reprod Biomed, Wenzhou 325000, Peoples R China
[3] Wenzhou Med Coll, Sch Pharm, Wenzhou 325000, Peoples R China
[4] Populat Council, New York, NY 10065 USA
[5] Rockefeller Univ, New York, NY 10065 USA
[6] Tongde Hosp Zhejiang Prov, Dept Pharm, Hangzhou 310007, Zhejiang, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 15期
关键词：
11; beta-HSD1; beta-HSD2; Mono-carbonyl curcumin analogues; Inhibitors; RAT LEYDIG-CELLS; BETA-HYDROXYSTEROID DEHYDROGENASE; IN-VITRO; TYPE-1; OBESITY; VIVO;
D O I：
10.1016/j.bmcl.2013.05.080
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of structurally novel mono-carbonyl curcumin analogues have been synthesized and biologically evaluated to test their inhibitory potencies and the structure-activity relationship (SAR) on human and rat 11 beta-hydroxysteroid dehydrogenase isoform (11 beta-HSD1) activities. 11 beta-HSD1 selective inhibitors have been discovered and compound A10 is discovered as a very potent with an IC50 value of 97 nM without inhibiting 11 beta-HSD2. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4362 / 4366
页数：5
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