Design, synthesis and anticancer screening of 3-(3-(substituted phenyl) acryloyl)-2H-chromen-2ones as selective anti-breast cancer agent
| Autor: | Afreen Begum, Swati A. Bhavale, Vishakha R. Shelke, Nikhil S. Sakle, Santosh N. Mokale |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Chalcone Nitrosourea medicine.drug_class Drug Evaluation Preclinical Antineoplastic Agents Pharmacology 01 natural sciences Rats Sprague-Dawley Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Breast cancer medicine Animals skin and connective tissue diseases Molecular Structure 010405 organic chemistry Mammary Neoplasms Experimental General Medicine medicine.disease Coumarin Rats 0104 chemical sciences 030104 developmental biology chemistry Docking (molecular) Estrogen Drug Design Female Pharmacophore Tamoxifen medicine.drug |
| Zdroj: | Biomedicine & Pharmacotherapy. 89:966-972 |
| ISSN: | 0753-3322 |
| DOI: | 10.1016/j.biopha.2017.02.089 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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