A novel type of retinoic acid receptor antagonist: synthesis and structure-activity relationships of heterocyclic ring-containing benzoic acid derivatives

H Yoshimura, M Nagai, S Hibi, K Kikuchi…

文献索引：Yoshimura; Nagai; Hibi; Kikuchi; Abe; Hida; Higashi; Yamanaka Journal of Medicinal Chemistry, 1995 , vol. 38, # 16 p. 3163 - 3173

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被引用次数: 49

摘要

A new series of heterocyclic ring-containing benzoic acids was prepared, and the binding affinity and antagonism of its members against all-trans-retinoic acid were evaluated by in vitro assay systems using human promyelocytic leukemia (HL-60) cells. Structure-activity relationships indicated that both an N-substituted pyrrole or pyrazole (1-position) and a hydrophobic region, with these linked by a ring system, were indispensable for effective ...