Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines

被引：42

作者：

Patel, Kuldeep ^{[1
]}

Karthikeyan, Chandrabose ^{[1
]}

Solomon, Viswas Raja ^{[2
,3
]}

Moorthy, N. S. Hari Narayana ^{[1
,4
]}

Lee, Hoyun ^{[2
,3
]}

Sahu, Kapendra ^{[1
]}

Deora, Girdhar Singh ^{[1
]}

Trivedi, Piyush ^{[1
]}

机构：

[1] Rajiv Gandhi Tech Univ, Sch Pharmaceut Sci, Bhopal 462036, MP, India

[2] Canada & Reg Hosp, NE Ontario Reg Canc Program Sudbury, Tumour Biol Grp, Sudbury, ON P3E 5J1, Canada

[3] Laurentian Univ, Dept Biol, Sudbury, ON P3E 2C6, Canada

[4] Univ Porto, Fac Sci, Dept Chem & Biochem, P-4169007 Oporto, Portugal

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2011年 / 8卷 / 04期

关键词：

Coumarinyl chalcones; Breast cancer cell lines; Antiproliferative activity; 184B5; CYTOTOXIC EVALUATION; P-GLYCOPROTEIN; DERIVATIVES; APOPTOSIS; AGENTS; ANTICANCER; INHIBITORS; GROWTH; ISOLIQUIRITIGENIN; PROLIFERATION;

D O I：

10.2174/157018011794839475

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R-1, R-2 and R-3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

引用

页码：308 / 311

页数：4

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