Synthesis, cytotoxicity, and anti-Trypanosoma cruzi activity of new chalcones

被引：109

作者：

Aponte, Jose C. ^{[1
]}

Verastegui, Manuela ^{[3
]}

Malaga, Edith ^{[3
]}

Zimic, Mirko ^{[2
]}

Quiliano, Miguel ^{[2
]}

Vaisberg, Abraham J. ^{[2
]}

Gilman, Robert H. ^{[4
]}

Hammond, Gerald B. ^{[1
]}

机构：

[1] Univ Louisville, Dept Chem, Louisville, KY 40292 USA

[2] Univ Peruana Cayetano Heredia, Fac Ciencias & Filosofia, Lab Invest & Desarrollo, Lima, Peru

[3] Univ Peruana Cayetano Heredia, Fac Ciencias & Filosofia, Dept Microbiol, Lima, Peru

[4] Johns Hopkins Univ, Sch Publ Hlth, Dept Int Hlth, Baltimore, MD 21205 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 19期

关键词：

D O I：

10.1021/jm800812k

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis of a cytotoxic dihydrochalcone, first isolated from a traditional Amazonian medicinal plant Iryanthera juruensis Warb (Myristicaceae), followed by a comprehensive SAR analysis of saturated and unsaturated chalcone synthetic intermediates, led to the identification of analogues with selective and significant in vitro anti-Trypanosoma cruzi activity. Further SAR studies were undertaken with the synthesis of 21 new chalcones containing two allyloxy moieties that resulted in the discovery of 2',4'-diallyloxy-6'-methoxy chalcones with improved selectivity against this parasite at concentrations below 25 mu M, four of which exhibited a selectivity index greater than 12.

引用

页码：6230 / 6234

页数：5

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