Synthesis and anticancer activity evaluation of 2(4-alkoxyphenyl)cyclopropyl hydrazides and triazolo phthalazines

被引：38

作者：

De, Prithwiraj ^{[1
,2
]}

Baltas, Michel ^{[1
,2
]}

Lamoral-Theys, Delphine ^{[3
]}

Bruyere, Celine ^{[4
]}

Kiss, Robert ^{[4
]}

Bedos-Belval, Florence ^{[1
,2
]}

Saffon, Nathalie ^{[5
]}

机构：

[1] Univ Toulouse, LSPCMIB, UPS, F-31062 Toulouse 9, France

[2] CNRS, LSPCMIB, F-31062 Toulouse 9, France

[3] Univ Libre Bruxelles, Inst Pharm, Lab Chim Analyt Toxicol & Chim Phys Appl, B-1050 Brussels, Belgium

[4] Univ Libre Bruxelles, Inst Pharm, Toxicol Lab, B-1050 Brussels, Belgium

[5] Univ Toulouse, UPS, FR 2599, F-31062 Toulouse 9, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 07期

关键词：

Cinnamic acid; Cyclopropyl backbone; Anticancer; Cytostatic activity; Apoptosis-resistant; CYTOTOXIC ACTIVITY; CYCLOPROPANATION; PROLIFERATION; INHIBITORS; RECEPTOR; DERIVATIVES; APOPTOSIS; ANTITUMOR; CELLS;

D O I：

10.1016/j.bmc.2010.02.041

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 new 2(4-alkoxyphenyl) cyclopropyl hydrazide-and triazolo-derivatives were synthesized starting from 4-hydroxycinnamic acid (1) in a clean, mild, efficient and straightforward synthetic protocol. These compounds consisting of different alkoxy substitution, phenylcyclopropyl backbone and different heterocyclic groups were evaluated for in vitro anticancer activity against 4 cell lines displaying certain levels of resistance to pro-apoptotic stimuli and 2 cell lines sensitive to pro-apoptotic compounds. Compounds 7f and 8e were most active and displaying moderate in vitro cytostatic effect through different mechanisms. Significantly, chemically modified derivatives could be obtained in order to develop novel types of compounds aiming to combat apoptosis-resistant cancers, for example, those cancers associated with dismal prognoses. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2537 / 2548

页数：12

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