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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Author(s): Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N. S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora and Piyush Trivedi

Volume 8, Issue 4, 2011

Page: [308 - 311] Pages: 4

DOI: 10.2174/157018011794839475

Price: $65


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 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.

Keywords: Coumarinyl chalcones, Breast cancer cell lines, Antiproliferative activity, 184B5, Cancer, Cardiovascular Disease, Skin Cancer, Therapeutic Strategies Monotherapy, Radiotherapy, Systemic Toxicity, Hetrocyclic, Non-heterocyclic Scaffolds, Antileishmanial

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