Novel Tricyclic Compounds Having Acetylene Groups at C-8a and Cyano Enones in Rings A and C: Highly Potent Anti-inflammatory and Cytoprotective Agents
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- 作者：Tadashi Honda ; Chitra Sundararajan ; Hidenori Yoshizawa ; Xiaobo Su ; Yukiko Honda ; Karen T. Liby ; Michael B. Sporn ; Gordon W. Gribble
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：April 19, 2007
- 年：2007
- 卷：50
- 期：8
- 页码：1731 - 1734
- 全文大小：119K
- 年卷期：v.50,no.8(April 19, 2007)
- ISSN：1520-4804
文摘
Novel C-8a functionalized tricyclic compounds having cyanoenones in rings A and C have been synthesized and biologicallyevaluated. Among them, compounds with acetylene groups at C-8ashow extremely high potency in in vitro and in vivo bioassays for anti-inflammatory and cytoprotective activities. Both in vitro and in vivopotencies are markedly higher than those of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), which is being evaluated as ananticancer drug in phase I clinical trials.