Literature DB >> 19740667

Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer.

Shailesh Kumar1, Shreekant Deshpande, Vishal Chandra, Shakti Kitchlu, Anila Dwivedi, Vadithe Lakshma Nayak, Rituraj Konwar, Yenamandra S Prabhakar, Devi Prasad Sahu.   

Abstract

A novel class of 2,3,4-triarylbenzopyrans has been synthesized and were evaluated for their selective estrogen receptor modulation activity and as a therapeutic agent for breast cancer. Among the compounds synthesized, compounds 11a and 12c exhibited 73.91% and 69.24% inhibition as estrogen antagonistic activity, respectively. Compound 12a showed the lowest IC(50) at 6.97 microM against MCF-7 and 11f showed the lowest IC(50) value of 5.6 microM against MDA-MB-231 cell line in spite of their low receptor binding affinity implicating these compounds probably act through ER independent mechanism.

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Year:  2009        PMID： 19740667     DOI： 10.1016/j.bmc.2009.08.034

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  4 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

2.  Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.

Authors:  Kevin Bonfield; Erica Amato; Tony Bankemper; Hannah Agard; Jeffrey Steller; James M Keeler; David Roy; Adam McCallum; Stefan Paula; Lili Ma
Journal:  Bioorg Med Chem       Date:  2012-02-27       Impact factor: 3.641

3.  Diastereoselective construction of 4-indole substituted chromans bearing a ketal motif through a three-component Friedel-Crafts alkylation/ketalization sequence.

Authors:  Jiao-Mei Guo; Wen-Bo Wang; Jia Guo; Yan-Shuo Zhu; Xu-Guan Bai; Shao-Jing Jin; Qi-Lin Wang; Zhan-Wei Bu
Journal:  RSC Adv       Date:  2018-04-25       Impact factor: 3.361

4.  Visible Light-Promoted Green and Sustainable Approach for One-Pot Synthesis of 4,4'-(Arylmethylene)bis(1H-pyrazol-5-ols), In Vitro Anticancer Activity, and Molecular Docking with Covid-19 Mpro.

Authors:  Anamika Gupta; Safia Iqbal; Mohd Kamil Hussain; Mohd Rehan Zaheer; Krapa Shankar
Journal:  ACS Omega       Date:  2022-09-14
  4 in total

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