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

Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N.S. Hari Narayana Moorthy, Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

Journal Article: Letters in Drug Design & Discovery 01/2011; 8:308-311.

Abstract

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 anti-proliferative activities. One of the compound 3i bearing methoxy substitutions at the R1, R2 and R3 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.

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