title: Design, synthesis and anticancer screening of 3-(3-(substituted phenyl) acryloyl)-2H-chromen-2ones as selective anti-breast cancer agent.
abstract: By utilizing concept of molecular hybridization, involving combination of various Pharmacophore, novel substituted coumarin-chalcone hybrids was synthesized and evaluated for anti-proliferative activity against estrogen receptor-positive MCF-7 and negative MDA-MB-435 breast cancer cell lines. In-vivo study was carried out by N-methyl nitrosourea (MNU) induced mammary carcinoma in virgin female Spraque Dawly (SD) rats. The compound 5b has highest potential than standard drug Adriamycin, comparable against Tamoxifen against ER-positive MCF-7 breast cancer cell lines. Docking study was performed to study the binding orientation and affinity of synthesized compounds on the ER-α enzyme.
authors.affiliation: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India. Electronic address: santoshmokale@rediffmail.com.
authors.forename: Santosh N
authors.initials: SN
authors.lastname: Mokale
authors.affiliation: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.
authors.forename: Afreen
authors.initials: A
authors.lastname: Begum
authors.affiliation: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.
authors.forename: Nikhil S
authors.initials: NS
authors.lastname: Sakle
authors.affiliation: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.
authors.forename: Vishakha R
authors.initials: VR
authors.lastname: Shelke
authors.affiliation: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, Maharashtra, India.
authors.forename: Swati A
authors.initials: SA
authors.lastname: Bhavale
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D005260:Female; D008325:Mammary Neoplasms, Experimental / Q000139:chemically induced / Q000188:drug therapy*; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents
keywords: Breast cancer; Chalcone; Coumarin; Molecular docking; SERM