Design, synthesis and evaluation of retinoids with novel bulky hydrophobic partial structures

Y Amano, M Noguchi, M Nakagomi, H Muratake…

Index: Amano, Yohei; Noguchi, Masayuki; Nakagomi, Madoka; Muratake, Hideaki; Fukasawa, Hiroshi; Shudo, Koichi Bioorganic and Medicinal Chemistry, 2013 ,  vol. 21,  # 14  p. 4342 - 4350

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Citation Number: 5

Abstract

Many synthetic retinoids contain an aromatic structure with a bulky hydrophobic fragment. In order to obtain retinoids with therapeutic potential that do not bind to or activate retinoic acid X receptors (RXRs), we focused on the introduction of novel hydrophobic moieties, that is, metacyclophane, phenalene and benzoheptalene derivatives. The designed compounds were synthesized and their agonistic activities towards RARs and RXRs were evaluated. ...