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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Research Article

Design and Synthesis of Some Novel Estrogen Receptor Modulators as Anti-Breast Cancer Agents: In Vitro & In Vivo Screening, Docking Analysis

Author(s): Pritam N. Dube and Santosh N. Mokale

Volume 16, Issue 11, 2016

Page: [1461 - 1467] Pages: 7

DOI: 10.2174/1871520616666160211124617

Price: $65

Abstract

A series of novel coumarin–chalcone hybrids have been synthesized in good yields and evaluated for their in vitro & in vivo anticancer activity. Cytotoxicity study was done against MCF-7 and Zr-75-1 human cancer cell lines. All compounds exhibited significant antiproliferative properties on both cell lines. The most active ER modulators found in in vitro screening are subjected for in vivo screened using methyl nitrosourea (MNU) induced mammary carcinoma in female spraque dawley rats. The Glide XP docking was performed for designed scaffold to optimize its structural requirement for ER-α inhibition.

Keywords: Breast cancer, estrogen receptor, chalcone-coumarin, docking.

Graphical Abstract


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