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 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
Letters in Drug Design & Discovery
Title: Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines
Volume: 8 Issue: 4
Author(s): Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N. S. Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora and Piyush Trivedi
Affiliation:
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
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 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.
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Cite this article as:
Patel Kuldeep, Karthikeyan Chandrabose, Raja Solomon Viswas, S. Hari Narayana Moorthy N., Lee Hoyun, Sahu Kapendra, Singh Deora Girdhar and Trivedi Piyush, Synthesis of Some Coumarinyl Chalcones and their Antiproliferative Activity Against Breast Cancer Cell Lines, Letters in Drug Design & Discovery 2011; 8 (4) . https://dx.doi.org/10.2174/157018011794839475
DOI https://dx.doi.org/10.2174/157018011794839475 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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