TY - JOUR
T1 - Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines
AU - Patel, Kuldeep
AU - Karthikeyan, Chandrabose
AU - Solomon, Viswas Raja
AU - Moorthy, N. S Hari Narayana
AU - Lee, Hoyun
AU - Sahu, Kapendra
AU - Deora, Girdhar Singh
AU - Trivedi, Piyush
PY - 2011/5
Y1 - 2011/5
N2 - 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.
AB - 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.
KW - 184B5
KW - Antiproliferative activity
KW - Breast cancer cell lines
KW - Coumarinyl chalcones
UR - http://www.scopus.com/inward/record.url?scp=79955943918&partnerID=8YFLogxK
U2 - 10.2174/157018011794839475
DO - 10.2174/157018011794839475
M3 - Article
AN - SCOPUS:79955943918
VL - 8
SP - 308
EP - 311
JO - Letters in Drug Design and Discovery
JF - Letters in Drug Design and Discovery
SN - 1570-1808
IS - 4
ER -