期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 12, 期 7, 页码 1027-1030出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00105-1
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资金
- NCI NIH HHS [R01-CA78814] Funding Source: Medline
New oleanane triterpenoids with various substituents at the C-17 position of 2-evano-3,12-dioxooleana-1,9(11)dien-28-oic acid (CDDO) and methyl 2-carboxy-3,12-dioxooleana-1,9(11)-dien-28-oate were synthesized. Among them, 2-cyano-3,12-dioxooleana- 1,9(11)-dien-28-onitrile shows extremely high inhibitory activity (IC50 = 1 pM level) against production of nitric oxide induced by interferon-gamma in mouse macrophages. This potency is about 100 times and 30 times more potent than CDDO and dexamethasone, respectively. (C) 2002 Elsevier Science Ltd. All rights reserved.
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