| Literature DB >> 12139443 |
Bitoku Takahashi1, Kiminori Ohta, Emiko Kawachi, Hiroshi Fukasawa, Yuichi Hashimoto, Hiroyuki Kagechika.
Abstract
Several 2-(arylamino)pyrimidine-5-carboxylic acids were designed as novel retinoid X receptor (RXR) antagonists. Compound 6a or 6b alone did not exhibit differentiation-inducing activity toward HL-60 cells and did not affect the activity of a retinoic acid receptor (RAR) agonist, Am80, but did inhibit the synergistic activity of an RXR agonist, PA024 (3), in the presence of Am80. The activity of 6 was ascribed to selective antagonism at the RXR site of RXR-RAR heterodimers.Entities:
Mesh：
Substances：
Year: 2002 PMID： 12139443 DOI： 10.1021/jm0255320
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446