Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596114 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
Based on structure-activity relationship studies of the benzoic acid part of diphenylamine-based retinoids, the potent RXR agonist 4 was derivatized to obtain retinoid agonists, synergists, and an antagonist. Cinnamic acid derivatives 5 and phenylpropionic acid derivatives 6 showed retinoid agonistic and synergistic activities, respectively. The difference of the activities is considered to be due to differences in the flexibility of the carboxylic acid-containing substituent on the diphenylamine skeleton. Compound 7, bearing a methyl group at the meta position to the carboxyl group, was an antagonist, dose-dependently inhibiting HL-60 cell differentiation induced by 3.3Â ÃÂ 10â10Â M Am80.
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Authors
Kiminori Ohta, Emiko Kawachi, Koichi Shudo, Hiroyuki Kagechika,