Synthesis and biological activity of retinoic acid receptor-α specific amides

被引:38
作者
Beard, RL [1 ]
Duong, TT
Teng, M
Klein, ES
Standevan, AM
Chandraratna, RAS
机构
[1] Allergan Pharmaceut Inc, Dept Chem, Retinoid Res, Irvine, CA 92623 USA
[2] Allergan Pharmaceut Inc, Dept Biol, Retinoid Res, Irvine, CA 92623 USA
关键词
D O I
10.1016/S0960-894X(02)00647-9
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and other serious hyperprolifierative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the design of retinoid receptor-alpha specific ligands with growth inhibitory activity in breast cancer cell lines, and which do not cause the cutaneous toxicity associated with the currently available nonselective retinoid agonists. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3145 / 3148
页数:4
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