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In‐vitro Antiproliferative Activity of Benzopyranone Derivatives in Comparison with Standard Chemotherapeutic Drugs
Author(s) -
Musa Musiliyu A.,
Cooperwood John S.,
Khan M. Omar F.,
Rahman Taufiq
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000207
Subject(s) - tamoxifen , chemistry , estrogen receptor , in vitro , pharmacology , in silico , cytotoxicity , raloxifene , mcf 7 , metabolite , cell culture , active metabolite , doxorubicin , stereochemistry , cancer cell , human breast , cancer , biochemistry , breast cancer , biology , medicine , chemotherapy , genetics , gene
The cytotoxic activities of five new benzopyranone derivatives containing basic amino side chain are described. Their cytotoxicities against ER(+) MCF‐7 and ER(–) MDA‐MB‐231 human breast cancer cell lines, and Ishikawa human endometrial cell line were determined after 72 h drug exposure employing CellTiter‐Glo assay at concentrations ranging from 0.01–1.0 × 10 5 nM. The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4‐hydroxytamoxifen (4‐OHT, active metabolite of tamoxifen), and raloxifene (RAL). In‐vitro results indicated that compounds 9 , 10 , 12 , and 13 were more potent than TAM against the human breast cancer cell lines with IC 50 < 20 µM. The in‐silico structure–activity relationships of these compounds and their binding mode within the estrogen receptor (ER) binding site using AutoDock vina are discussed.