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, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

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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. 

Original languageEnglish
Pages (from-to)308-311
Number of pages4
JournalLetters in Drug Design and Discovery
Issue number4
Publication statusPublished - May 2011
Externally publishedYes


  • 184B5
  • Antiproliferative activity
  • Breast cancer cell lines
  • Coumarinyl chalcones

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