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Diphenylamine-based retinoid antagonists: Regulation of RAR and RXR function depending on the N-substituent
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DOI：10.1016/j.bmc.2011.03.026.png)
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Abstract
En 中文
Based upon the structure-activity relationships of diphenylamine derivatives with retinoid synergistic activity (RXR agonists), novel diphenylamine derivatives with a long alkyl chain (9a and 9b) or a benzyl group (10a-f) as the N-substituent were designed and synthesized. All the synthesized compounds dose-dependently inhibited HL-60 cell differentiation induced by 3.3 x 10 (10) M Am80. Among them, compound 10f showed the most potent inhibitory activity, and the mechanism was shown, by means of transactivation assay for RARs and RXRs, to involve antagonism against RARs. The N-substituent of the diphenylamine skeleton plays an important role in determining the receptor selectivity for RARs or RXRs, as well as the agonist or antagonist nature of the activity. (C) 2011 Elsevier Ltd. All rights reserved.
Keywords:
Retinoid
RAR
Antagonist
Diphenylamine
Journal
B
IF:
3
Papers:
1.7W
Citations:
2.7W
Organization
Cited Papers