國家衛生研究院 NHRI:Item 3990099045/5207

NHRI > Institute of Biotechnology and Pharmaceutical Research > Yu-Sheng Chao(2002-2013) > Periodical Articles > Item 3990099045/5207

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/5207

Title:	Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents
Authors:	Li, WT;Hwang, DR;Song, JS;Chen, CP;Chen, TW;Lin, CH;Chuu, JJ;Lien, TW;Hsu, TA;Huang, CL;Tseng, HY;Lin, CC;Lin, HL;Chang, CM;Chao, YS;Chen, CT
Contributors:	Institute of Biotechnology and Pharmaceutical Research;Division of Molecular and Genomic Medicine
Abstract:	Designed from a high throughput screened hit compound, novel 2-amino-1-thiazolyl imidazoles were synthesized and demonstrated cytotoxicity against human cancer cells. 1-(4-Phenylthiazol-2-yl)-4-(thiophen-2-yl)-1H-imidazol-2-amine (compound 2), a 2-amino-1-thiazolyl imidazole, inhibited tubulin polymerization, interacted with the colchicine-binding sites of tubulins, and caused cell cycle arrest at the G(2)/M phase in human gastric cancer cells. Disruption of the microtubule structure in cancer cells by compound 2 was also observed. Compound 2 concentration-dependently inhibited the proliferation of cancer cells in histocultured human gastric and colorectal tumors. Given orally, compound 2 prolonged the lifespans of leukemia mice intraperitoneally inoculated with the murine P388 leukemic cells. We report 2-amino-1-thiazolyl imidazoles as a novel class of orally active microtubule-destabilizing anticancer agents.
Date:	2012-02
Relation:	Investigational New Drugs. 2012 Feb;30(1):164-175.
Link to:	http://dx.doi.org/10.1007/s10637-010-9547-7
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0167-6997&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000299121500017
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84856526521
Appears in Collections:	[Yu-Sheng Chao(2002-2013)] Periodical Articles [John Tsu-An Hsu] Periodical Articles [Chiung-Tong Chen] Periodical Articles [Chung-Ming Chang] Periodical Articles

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