國家衛生研究院 NHRI:Item 3990099045/4065
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    題名: Synthesis and biological activities of 2-Amino-1-arylidenamino imidazoles as orally active anticancer agents
    作者: Li, WT;Hwang, DR;Song, JS;Chen, CP;Chuu, JJ;Hu, CB;Lin, HL;Huang, CL;Huang, CY;Tseng, HY;Lin, CC;Chen, TW;Lin, CH;Wang, HS;Shen, CC;Chang, CM;Chao, YS;Chen, CT
    貢獻者: Division of Biotechnology and Pharmaceutical Research;Division of Molecular and Genomic Medicine
    摘要: 2-Amino-1-arylidenaminoimidazoles, a novel class of orally (po) active microtubule-destabilizing anticancer agents, were synthesized. The compounds were designed from a hit compound identified in a drug discovery platform by using cancer cell-based high throughput screening assay. Selective synthesized compounds exerted cell cytotoxicity against human cancer cells. The underlying mechanisms for the anticancer activity were demonstrated as interacting with the tubulins and inhibiting microtubule assembly, leading to proliferation inhibition and apoptosis induction in the human tumor cells. Furthermore, two compounds showed in vivo anticancer activities in both po and intravenously (iv) administered routes and prolonged the life spans of murine leukemic P388 cells-inoculated mice. These new po active antimitotic anticancer agents are to be further examined in preclinical studies and developed for clinical uses.
    日期: 2010-03
    關聯: Journal of Medicinal Chemistry. 2010 Mar;53(6):2409-2417.
    Link to: http://dx.doi.org/10.1021/jm901501s
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000275711000009
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77949859258
    顯示於類別:[陳炯東] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [張仲明] 期刊論文

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