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Anticancer Agents Med Chem. 2019 Mar 7. doi: 10.2174/1871520619666190307121145. [Epub ahead of print]

Synthesis, Biological Investigation and Docking Study of Novel Chromen Derivatives as Anti-Cancer Agents.

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Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad-431001, Maharashtra. India.


A series of novel 6-methyl-3-(3-oxo-1-phenyl-3-(4-(2-(piperidin-1-yl)ethoxy)phenyl)propyl)-2H-chromen-2-one was designed, synthesized and screened for their Anti-Breast Cancer activity against estrogen receptor-positive MCF-7, ZR-75-1 and negative MDA-MB-435 human breast cancer cell lines. Among the synthesized compounds C-3, C-5 and C-15 were showing potent cytotoxicity against estrogen receptor-positive MCF-7. The potent cytotoxic compounds C-3, C-5 and C-15 were further evaluated for in vivo anti-cancer activity by MNU (N-methyl-N-nitrosourea) induced mammary carcinoma in female Sprague-Dawley rats. The in vivo anti-cancer activity result shows that the compound C-5 has protuberant affinity towards estrogen receptor as standard TAM (tamoxifen). The docking study was performed to predict binding orientation towards the estrogen receptor-α. The designed class has very promising starting point for the development and further improvement in anti-breast cancer class of drugs.


Breast cancer; SERMs; anti-cancer agents; chalcone; docking; novel chromen derivatives

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