Diphenyleyclohexylamine derivatives as new potent multidrug resistance (MDR) modulators

被引：13

作者：

Dei, S

Budriesi, R

Sudwan, P

Ferraroni, M

Chiarini, A

Garnier-Suillerot, A

Manetti, D

Martelli, C

Scapecchi, S

Teodori, E

机构：

[1] Univ Florence, Dipartimento Sci Farmaceut, I-50019 Sesto Fiorentino, FI, Italy

[2] Univ Florence, Dipartimento Chim, I-50019 Sesto Fiorentino, FI, Italy

[3] Univ Paris 13, Lab Physicochim Biomol & Cellulaire, UMR 7033, F-93017 Bobigny, France

[4] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 04期

关键词：

multidrug resistance (MDR); MDR modulators; chemosensitizer; diphenylcyclohexylamine derivatives;

D O I：

10.1016/j.bmc.2004.11.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of compounds with a diphenylmethyl cyclohexyl skeleton, loosely related to verapamil, has been synthesized and tested as MDR modulators on anthracycline-resistant erythroleukemia K 562 cells. Their residual cardiovascular action (negative inotropic and chronotropic activity as well as vasorelaxant activity) was evaluated on guinea-pig isolated atria preparations and on guinea-pig aortic strip preparations. Most compounds of the series possess a good MDR-reverting activity together with a low cardiovascular action. Among them, compounds 3a(1), 7a, and 8a are more potent than verapamil as MDR reverters and lack any cardiovascular action; they can represent useful leads for the development of new safe MDR reversing drugs. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：985 / 998

页数：14

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