Novel synthetic oleanane triterpenoids: A series of highly active inhibitors of nitric oxide production in mouse macrophages

Novel synthetic oleanane triterpenoids: A series of highly active inhibitors of nitric oxide production in mouse macrophages
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DOI:
10.1016/s0960-894x(99)00623-x
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发表时间:
1999-12-20
影响因子:
2.7
通讯作者:
Sporn, MB
Sporn, MB
中科院分区:
医学4区
文献类型:
--
作者:
Honda, T;Rounds, BV;Sporn, MB

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设计并合成了具有A和C环修饰的新型齐墩烷三萜。其中,甲基2-羧基-3,12-二氧齐烷-1,9-二烯-28-oic酸与我们之前合成的2-氰基-3,12-二氧齐烷-1,9-二烯-28-oic酸(CDDO)对干扰素γ诱导的小鼠巨噬细胞产生一氧化氮具有相似的高抑制活性(IC50 = 0.8 nM)。1999爱思唯尔科学有限公司版权所有。
Novel oleanane triterpenoids with modified rings A and C were designed and synthesized. Among them, methyl 2-carboxy-3,12-dioxooleana-1,9-dien-28-oate showed similar high inhibitory activity (IC50 = 0.8 nM) to 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO), which we have synthesized previously, against production of nitric oxide induced by interferon-gamma in mouse macrophages. (C) 1999 Elsevier Science Ltd. All rights reserved.