Abstract

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.

Graphical Abstract