Retinoid X receptor-antagonistic diazepinylbenzoic acids.

  title={Retinoid X receptor-antagonistic diazepinylbenzoic acids.},
  author={Michiko Ebisawa and Hiroki Umemiya and Katsuki Ohta and Hiroshi Fukasawa and Emiko Kawachi and G Christoffel and Hinrich Gronemeyer and Masao Tsuji and Yuichi Hashimoto and Koichi Shudo and Hiroyuki Kagechika},
  journal={Chemical & pharmaceutical bulletin},
  volume={47 12},
Several dibenzodiazepine derivatives were identified as novel retinoid X receptor (RXR) antagonists on the basis of inhibitory activity on retinoid-induced cell differentiation of human promyelocytic leukemia cells HL-60 and transactivation assay using retinoic acid receptors (RARs) and RXRs in COS-1 cells. 4-(5H-2,3-(2,5-Dimethyl-2,5-hexano)-5-n- propyldibenzo[b,e][1,4]diazepin-11-yl)benzoic acid (HX603, 6c) is an N-n-propyl derivative of an RXR pan-agonist HX600 (6a), and exhibited RXR… CONTINUE READING


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