Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues

被引：50

作者：

Youssef, Dani

Nichols, Christie E.

Cameron, T. Stanley

Balzarini, Jan

De Clercq, Erik

Jha, Amitabh ^{[1
]}

机构：

[1] Acadia Univ, Dept Chem, Wolfville, NS B4P 2R6, Canada

[2] Univ Sainte Anne, Dept Sci, Church Point, NS B0W 1M0, Canada

[3] Dalhousie Univ, Dept Chem, Halifax, NS B3H 4J3, Canada

[4] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 20期

基金：

加拿大自然科学与工程研究理事会;

关键词：

curcumin analogues; cytostatic activity; anticancer; QSAR; anti-oxidant;

D O I：

10.1016/j.bmcl.2007.07.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel cyclic analogues of curcumin were synthesized and analyzed for in vitro cytostatic activity. Condensation of 2-acetylcycloalkanones with a variety of aromatic aldehydes resulted in the formation of 2-arylidene-6-(3-arylacryoyl)-cyclo-alkanone derivatives. A number of these analogues were found to have significant anticancer activity against representative murine and human cancer cell lines during in vitro bioassays. This corroborated with in vitro cytostatic activity against a panel of 60 cell lines studied at the National Cancer Institute (USA). (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5624 / 5629

页数：6

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[1] Synthesis and biological evaluation of novel curcumin analogs as anti-cancer and anti-angiogenesis agents [J].