Design and synthesis of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid, a novel and highly active inhibitor of nitric oxide production in mouse macrophages
Design and synthesis of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid, a novel and highly active inhibitor of nitric oxide production in mouse macrophages
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DOI：
10.1016/s0960-894x(98)00479-x
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发表时间：
1998-10-06
影响因子：
2.7
通讯作者：
Sporn, MB
中科院分区：
文献类型：
--
作者：
Honda, T;Rounds, BV;Sporn, MB
合成了3-氧代-1-烯-28-酸的C-2位含吸电子取代基的新衍生物。其中，2-氰基-3，12-二氧杂环戊烯-1，9-二烯-28-酸(CDDO)对干扰素-γ诱导的小鼠巨噬细胞产生一氧化氮的抑制作用(IC50，0.4 nM)是我们合成的化合物的400倍。CDDO的药效与地塞米松相似，尽管CDDO不通过糖皮质激素受体发挥作用。(C)1998爱思唯尔科学有限公司。保留所有权利。
New derivatives with electron-withdrawing substituents at the C-2 position of 3-oxoolean-1-en-28-oic acid were synthesized. Among them, 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid (CDDO) was 400 times more potent than previous compounds we have made as an inhibitor of production of nitric oxide induced by interferon-gamma in mouse macrophages (IC50, 0.4 nM). The potency of CDDO was similar to that of dexamethasone, although CDDO does not act through the glucocorticoid receptor. (C) 1998 Elsevier Science Ltd. All rights reserved.