1416255-02-1Relevant articles and documents
Structure-activity relationship study on benzoic acid part of diphenylamine-based retinoids
Ohta, Kiminori,Kawachi, Emiko,Shudo, Koichi,Kagechika, Hiroyuki
, p. 81 - 84 (2013/02/23)
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 3.3 × 10-10 M Am80.