Regulation of retinoidal actions by diazepinylbenzoic acids. 1 retinoid synergists which activate the RXR-RAR heterodimers

…, E Kawachi, G Eisenmann, H Gronemeyer…

Index: Umemiya, Hiroki; Fukasawa, Hiroshi; Ebisawa, Masayuki; Eyrolles, Laurence; Kawachi, Emiko; Eisenmann, Ghislaine; Gronemeyer, Hinrich; Hashimoto, Yuichi; Shudo, Koichi; Kagechika, Hiroyuki Journal of Medicinal Chemistry, 1997 , vol. 40, # 26 p. 4222 - 4234

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Citation Number: 152

Abstract

In human HL-60 promyelocytic leukemia cells, diazepinylbenzoic acid derivatives can exhibit either antagonistic or synergistic effects on the differentiation-inducing activities of natural or synthetic retinoids, the activity depending largely on the nature of the substituents on the diazepine ring. Thus, a benzolog of the retinoid antagonist LE135 (6), 4-(13 H-10, 11, 12, 13-tetrahydro-10, 10, 13, 13, 15-pentamethyldinaphtho [2, 3-b][1, 2-e] diazepin-7-yl) ...