Synthesis,in Vitro,and in Vivo Biological Evaluation and Molecular Docking Analysis of Novel 3‐(3‐oxo‐substitutedphenyl‐3‐)4‐(2‐(piperidinyl)ethoxy)phenyl)propyl)‐2H‐chromen‐2‐one Derivatives as Anti‐breast Cancer Agents |
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| Authors: | Pritam N. Dube Madhuri N. Waghmare Santosh N. Mokale |
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| Affiliation: | Department of Pharmaceutical Chemistry, Y. B. Chavan College of Pharmacy, Aurangabad, Maharashtra, India |
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| Abstract: | The analogs of coumarin–chalcones have been reported to exhibit antineoplastic, anti‐allergic, antihepatoprotective, and estrogenic activity. Herein, we have reported 3‐(3‐oxo‐substitutedphenyl‐3‐)4‐(2‐(piperidinyl)ethoxy)phenyl)propyl)‐2H‐chromen‐2‐one derivatives as a new class of compounds that exhibit selectivity for ER‐α binding along with antiproliferative and cytotoxic activity on human breast cancer cell line. The active compounds which show prominent activity against estrogen receptor‐alpha‐positive (ER+) human breast cancer cell lines MCF‐7 and Zr‐75‐1 are subjected to in vivo screening. The Glide XP docking was performed for designed scaffold to optimize its structural requirement for ER‐α inhibition. |
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| Keywords: | breast cancer Coumarin– chalcone docking estrogen receptor |
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