期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 16, 页码 3327-3330出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm0255320
关键词
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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.
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