کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1356178 981096 2011 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Diphenylamine-based retinoid antagonists: Regulation of RAR and RXR function depending on the N-substituent
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Diphenylamine-based retinoid antagonists: Regulation of RAR and RXR function depending on the N-substituent
چکیده انگلیسی

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 × 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.

N-Benzylated diphenylamine derivative 10f potently inhibited Am80-induced HL-60 cell differentiation as a result of RAR-antagonistic action.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 8, 15 April 2011, Pages 2501–2507
نویسندگان
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