具有类视黄醇协同活性的新型噻唑烷二酮衍生物。
Novel thiazolidinedione derivatives with retinoid synergistic activity.
作者信息
Ebisawa M, Kawachi E, Fukasawa H, Hashimoto Y, Itai A, Shudo K, Kagechika H
机构信息
Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
出版信息
Biol Pharm Bull. 1998 May;21(5):547-9. doi: 10.1248/bpb.21.547.
PMID:9635519
Abstract
Several arylmethylidene thiazolidinediones were synthesized and their retinoidal activities were examined. TZ181 (7a), having a benzanilide skeleton, exhibited differentiation-inducing activity in HL-60 cell assay, while TZ191 (7b), the N-methylated analog of TZ181 (7a), TZ245 (9) and TZ335 (10) acted as retinoid synergists like the RXR-selective ligand, LGD1069 (5).
摘要
合成了几种芳基亚甲基噻唑烷二酮，并检测了它们的类视黄醇活性。具有苯甲酰苯胺骨架的TZ181（7a）在HL-60细胞试验中表现出诱导分化活性，而TZ181（7a）的N-甲基化类似物TZ191（7b）、TZ245（9）和TZ335（10）像RXR选择性配体LGD1069（5）一样作为类视黄醇增效剂发挥作用。
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