Synthesis and structure-activity analysis of novel dihydropyridine derivatives to overcome multidrug resistance

被引：65

作者：

Tasaka, S

Ohmori, H

Gomi, N

Iino, M

Machida, T

Kiue, A

Naito, S

Kuwano, M

机构：

[1] Nikken Chem Co Ltd, Omiya Res Lab, Omiya, Saitama 3300835, Japan

[2] Kyushu Univ, Grad Sch Med Sci, Dept Urol, Higashi Ku, Fukuoka 8128582, Japan

[3] Kyushu Univ, Grad Sch Med Sci, Dept Biochem, Higashi Ku, Fukuoka 8128582, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(00)00651-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-activity relationships were studied on newly synthesized 1,4-dihydropyridine derivatives possessing a 1-pentyl group at the 4-position, and 3-pyridylpropylester was found to be one of the effective fragments for overcoming P-glycoprotein mediated multidrug-resistance (MDR) in cultured human cancer cells, in vitro. 3-Pyridylpropylester was also found to be one of the effective fragments for increasing the life span of P-glycoprotein overexpressing MDR P388 leukemia-bearing mice, in vivo. All compounds had weak calcium antagonistic activities, but there appeared no relationship between MDR reversing effect and calcium antagonistic activity. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：275 / 277

页数：3

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