國家衛生研究院 NHRI:Item 3990099045/5207
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    题名: Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents
    作者: 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
    贡献者: Institute of Biotechnology and Pharmaceutical Research;Division of Molecular and Genomic Medicine
    摘要: 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.
    日期: 2012-02
    關聯: 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
    显示于类别:[趙宇生(2002-2013)] 期刊論文
    [徐祖安] 期刊論文
    [陳炯東] 期刊論文
    [張仲明] 期刊論文

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