Design, synthesis and anticancer screening of 3-(3-(substituted phenyl) acryloyl)-2H-chromen-2ones as selective anti-breast cancer agent - 25/04/17
, Afreen Begum, Nikhil S. Sakle, Vishakha R. Shelke, Swati A. BhavaleBienvenue sur EM-consulte, la référence des professionnels de santé.
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Graphical abstract |
Highlights |
• | By utilizing concept of molecular hybridization novel coumarin-chalcone derivatives were synthesized. |
• | The synthesized derivatives were evaluated for anti-proliferative activity. |
• | The in-vivo study was performed using MNU induced mammary carcinoma in female spraque dawly rats. |
• | The compound 5b has highest potential than standard drug Adriamycin and comparable against Tamoxifen. |
• | Docking study was performed to study the binding orientation and affinity of synthesized compounds for ER-α enzyme. |
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.
Le texte complet de cet article est disponible en PDF.Keywords : Coumarin, Chalcone, SERM, Breast cancer, Molecular docking
Plan
Vol 89
P. 966-972 - mai 2017 Retour au numéro
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