Literature DB >> 25899332

Design and optimization of hybrid of 2,4-diaminopyrimidine and arylthiazole scaffold as anticancer cell proliferation and migration agents.

Wenbo Zhou1, Anling Huang1, Yong Zhang1, Qingxiang Lin1, Weikai Guo1, Zihua You1, Zhengfang Yi1, Mingyao Liu1, Yihua Chen2.   

Abstract

Therapeutics of metastatic or triple-negative breast cancer are still challenging in clinical. Herein we demonstrated the design and optimization of a series of hybrid of 2,4-diaminopyrimidine and arylthiazole derivatives for their anti-proliferative properties against two breast cancer cell lines (MCF-7 as human breast cancer and MDA-MB-231 as triple-negative breast cancer). More importantly, some of those compounds with potent antiproliferative activities also indicated excellent inhibitory activities against MDA-MB-231 cell migration. These results suggested that the new series of hybridation of aryl-thiazoles and aminopyrimidines could be identified and developed as novel highly potential anticancer agents against the triple-negative breast cancer as well as metastatic one in the future.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Aminopyrimidines; Antitumor growth and metastasis; Arylthiazoles; Hybridation; Structure–activity relationships

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Year:  2015        PMID: 25899332     DOI: 10.1016/j.ejmech.2015.04.027

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Discovery and Optimization of N-Substituted 2-(4-pyridinyl)thiazole carboxamides against Tumor Growth through Regulating Angiogenesis Signaling Pathways.

Authors:  Wenbo Zhou; Wenshu Tang; Zhenliang Sun; Yunqi Li; Yanmin Dong; Haixiang Pei; Yangrui Peng; Jinhua Wang; Ting Shao; Zhenran Jiang; Zhengfang Yi; Yihua Chen
Journal:  Sci Rep       Date:  2016-09-16       Impact factor: 4.379

2.  Crystal structures and Hirshfeld surface analyses of 2-[(4,6-di-amino-pyrimidin-2-yl)sulfan-yl]-N-(pyridin-2-yl)acetamide and 2-[(4,6-di-amino-pyrimidin-2-yl)sulfan-yl]-N-(pyrazin-2-yl)acetamide.

Authors:  Manisha Choudhury; Vijayan Viswanathan; Ajay Kumar Timiri; Barij Nayan Sinha; Venkatesan Jayaprakash; Devadasan Velmurugan
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2018-04-27

3.  Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression.

Authors:  Qingxiang Lin; Yuan He; Xue Wang; Yong Zhang; Meichun Hu; Weikai Guo; Yundong He; Tao Zhang; Li Lai; Zhenliang Sun; Zhengfang Yi; Mingyao Liu; Yihua Chen
Journal:  Adv Sci (Weinh)       Date:  2020-03-12       Impact factor: 16.806

  3 in total

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