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
Anti-Cancer Agents in Medicinal Chemistry
Title:Design and Synthesis of Some Novel Estrogen Receptor Modulators as Anti-Breast Cancer Agents: In Vitro & In Vivo Screening, Docking Analysis
Volume: 16 Issue: 11
Author(s): Pritam N. Dube and Santosh N. Mokale
Affiliation:
Keywords: Breast cancer, estrogen receptor, chalcone-coumarin, docking.
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.
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Cite this article as:
Dube N. Pritam and Mokale N. Santosh, Design and Synthesis of Some Novel Estrogen Receptor Modulators as Anti-Breast Cancer Agents: In Vitro & In Vivo Screening, Docking Analysis, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (11) . https://dx.doi.org/10.2174/1871520616666160211124617
DOI https://dx.doi.org/10.2174/1871520616666160211124617 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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