Novel retinoidal tropolone derivatives. Bioisosteric relationship of tropolone ring with benzoic acid moiety in retinoid structure

被引：26

作者：

Ebisawa, M

Ohta, K

Kawachi, E

Fukasawa, H

Hashimoto, Y

Kagechika, H

机构：

[1] Univ Tokyo, Grad Sch Pharmaceut Sci, Bunkyo Ku, Tokyo 1130033, Japan

[2] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2001年 / 49卷 / 04期

关键词：

retinoid; tropolone; bioisoster; cell differentiation;

D O I：

10.1248/cpb.49.501

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several tropolone derivatives (4-7) were designed as novel retinoids on the assumption that the tropolone ring may mimic the benzoic acid moiety in retinoid structures, such as Am80 (2), Among the synthesized compounds, 5-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)ethynyl] tropolone (7a) showed moderate potency as a differentiation-inducer of HL-60 cells. The activities of the tropolones were greatly enhanced in the presence of HX630, an RXR agonist (retinoid synergist).

引用

页码：501 / 503

页数：3

共 20 条

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