國家衛生研究院 NHRI:Item 3990099045/4065

NHRI > Institute of Biotechnology and Pharmaceutical Research > Chiung-Tong Chen > Periodical Articles > Item 3990099045/4065

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/4065

Title:	Synthesis and biological activities of 2-Amino-1-arylidenamino imidazoles as orally active anticancer agents
Authors:	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
Contributors:	Division of Biotechnology and Pharmaceutical Research;Division of Molecular and Genomic Medicine
Abstract:	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.
Date:	2010-03
Relation:	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
Appears in Collections:	[Chiung-Tong Chen] Periodical Articles [Yu-Sheng Chao(2002-2013)] Periodical Articles [Chung-Ming Chang] Periodical Articles

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