2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸的设计与合成，一种新型且高效的小鼠巨噬细胞中一氧化氮产生的抑制剂。
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.
作者信息
Honda T, Rounds B V, Gribble G W, Suh N, Wang Y, Sporn M B
机构信息
Department of Chemistry, Dartmouth College, Hanover, NH 03755, USA.
出版信息
Bioorg Med Chem Lett. 1998 Oct 6;8(19):2711-4. doi: 10.1016/s0960-894x(98)00479-x.
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.
合成了在3-氧代齐墩果-1-烯-28-酸的C-2位带有吸电子取代基的新型衍生物。其中，2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸（CDDO）作为小鼠巨噬细胞中干扰素-γ诱导的一氧化氮产生的抑制剂，其效力比我们之前制备的化合物高400倍（IC50，0.4 nM）。尽管CDDO不通过糖皮质激素受体起作用，但其效力与地塞米松相似。
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