Document Report Card

ID: ALA1133462

Journal: J Med Chem

Title: Discovery of novel and potent retinoic acid receptor alpha agonists: syntheses and evaluation of benzofuranyl-pyrrole and benzothiophenyl-pyrrole derivatives.

Authors: Yoshimura H, Kikuchi K, Hibi S, Tagami K, Satoh T, Yamauchi T, Ishibahi A, Tai K, Hida T, Tokuhara N, Nagai M.

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.

CiteXplore: 10956201

DOI: 10.1021/jm000098s