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, Santosh N. Mokale.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 16 , Issue 11 , 2016

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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.

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Article Details

VOLUME: 16
ISSUE: 11
Year: 2016
Page: [1461 - 1467]
Pages: 7
DOI: 10.2174/1871520616666160211124617
Price: $58

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