Discovery of novel and potent retinoic acid receptor alpha agonists: syntheses and evaluation of benzofuranyl-pyrrole and benzothiophenyl-pyrrole derivatives |
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| Authors: | Yoshimura H Kikuchi K Hibi S Tagami K Satoh T Yamauchi T Ishibahi A Tai K Hida T Tokuhara N Nagai M |
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| Affiliation: | Tsukuba Basic Research Laboratories for Drug Discovery, Eisai Company, Ltd., Ibaraki, Japan. |
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| Abstract: | In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of benzofuran and benzothiophene derivatives. Some of these compounds (1a,b,e,f,j) markedly inhibited LPS-induced B-lymphocyte proliferation and exerted RARalpha selectivity. One of them, 4-[5-(4,7-dimethylbenzofuran-2-yl)pyrrol-2-yl]benzoic acid (1b), when orally administered significantly inhibited mouse antibody production and delayed type hypersensitivity (DTH) responses from a dose of 0.1 mg/kg. |
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