Novel tricyclic compounds having acetylene groups at C-8a and cyano enones in rings A and C: Highly potent anti-inflammatory and cytoprotective agents

被引：27

作者：

Honda, Tadashi ^{[1
]}

Sundararajan, Chitra

Yoshizawa, Hidenori

Su, Xiaobo

Honda, Yukiko

Liby, Karen T.

Sporn, Michael B.

Gribble, Gordon W.

机构：

[1] Dartmouth Coll, Dept Chem, Burke Lab 6128, Hanover, NH 03755 USA

[2] Dartmouth Coll Sch Med, Dept Pharmacol & Toxicol, Hanover, NH 03755 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 08期

关键词：

D O I：

10.1021/jm070141c

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel C-8a functionalized tricyclic compounds having cyano enones in rings A and C have been synthesized and biologically evaluated. Among them, compounds with acetylene groups at C-8a show extremely high potency in in vitro and in vivo bioassays for anti-inflammatory and cytoprotective activities. Both in vitro and in vivo potencies are markedly higher than those of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), which is being evaluated as an anticancer drug in phase I clinical trials.

引用

页码：1731 / 1734

页数：4

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