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Design and Synthesis of Novel Chalcone-Phenylpyranone Derivatives as Estrogen Receptor Modulators

1
Department of Pharmaceutical Chemistry, SNJB’s SSD Jain College of Pharmacy, Neminagar, Chandwad, Nashik 423101, Maharashtra, India
2
Department of Pharmaceutical Chemistry, MET Institute of Pharmacy, Bhujbal Knowledge City, Adgaon, Nashik 422003, Maharashtra, India
*
Author to whom correspondence should be addressed.
Presented at the 22nd International Electronic Conference on Synthetic Organic Chemistry, 15 November–15 December 2018; Available Online: https://sciforum.net/conference/ecsoc-22for every paper.
Proceedings 2019, 9(1), 30; https://doi.org/10.3390/ecsoc-22-05874
Published: 23 November 2018
PDF [546 KB, uploaded 21 March 2019]

Abstract

Selective estrogen receptor modulators (SERMs) are a class of drugs that act on the estrogen receptor (ER). SERMs are used for treatment and reduction of risk of breast cancer. Herewith we had designed, synthesized, and evaluated chalcone-phenylpyran-2-one derivatives bearing a N,N-dimethyl ethylamine side chain for their anti-breast cancer activity on MCF-7 and Zr-75-1 cell lines in-vitro. The pharmacological data indicated that most of tested compounds showed moderate to significant cytotoxicity and high selectivity toward the estrogen receptor. The Structure activity relationaship analyses indicated that compounds 5f with 2,6-dichloro substitution was more effective. Docking study was performed to predict binding orientation towards the estrogen receptor-α.
Keywords: Breast cancer; Chalcone; Docking; MCF-7; Phenylpyranone; SERM; Breast cancer; Chalcone; Docking; MCF-7; Phenylpyranone; SERM;
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Dube, P.N.; Thombare, Y.B.; Chatpalliwar, V.A. Design and Synthesis of Novel Chalcone-Phenylpyranone Derivatives as Estrogen Receptor Modulators. Proceedings 2019, 9, 30.

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