A series of novel coumarin–chalcone hybrids have been synthesized in good yields
and evaluated for their in vitro & in vivo anticancer activity. Cytotoxicity study was done
against MCF-7 and Zr-75-1 human cancer cell lines. All compounds exhibited significant
antiproliferative properties on both cell lines. The most active ER modulators found in in vitro
screening are subjected for in vivo screened using methyl nitrosourea (MNU) induced mammary
carcinoma in female spraque dawley rats. The Glide XP docking was performed for designed
scaffold to optimize its structural requirement for ER-α inhibition.
Keywords: Breast cancer, estrogen receptor, chalcone-coumarin, docking.
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