title: Design and Synthesis of Some Novel Estrogen Receptor Modulators as Anti-Breast Cancer Agents: In Vitro & In Vivo Screening, Docking Analysis.
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.
authors: Pritam N
authors: PN
authors: Dube
authors: Dr. Rafiq Zakaria Campus, Y. B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.
authors: Santosh N
authors: SN
authors: Mokale
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D020847:Estrogen Receptor Modulators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D020847:Estrogen Receptor Modulators