6-Alkylamino-2-(3-hydroxyphenyl)quinoIin-4-one Derivatives Induced Mitotic Arrest in Human Hep3B Cells

CNU IR > Pharmacy and Science > 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium > Item 310902800/24228

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Title:	6-Alkylamino-2-(3-hydroxyphenyl)quinoIin-4-one Derivatives Induced Mitotic Arrest in Human Hep3B Cells
Authors:	Mei-Hua Hsu (徐美華) Li-Chen Chou (周立琛) Ming-Hua Chen (陳明華) Chi-Hung Huang (黃濟鴻) Hui-Yi Lin (林慧怡) Shi-Hon Zhuang (莊仕弘) Chien-Ting Chen (陳建廷) Li-Jiau Huang (黃麗嬌) Sheng-Chu Kuo ()
Date:	2011
Issue Date:	2011-06-23 14:57:19 (UTC+8)
Abstract:	In order to develop potential backup compounds for our previous identified new anticancer drug candidate,CHM-l-P-Na, a series of 6-alkylamino-2-(3-hydroxyphenyl)quinolin-4-one derivatives were designed and synthesized. The newly synthesized derivatives were evaluated for cytotoxicity and structure-activity relationships were established. Among those tested compounds, 6-pyrrolidino-2-(3-hydroxyphenyl)quinolin-4-one (A) was the most promising agent which was submitted to NCI for evaluation against 60 human cancer cell lines. Furthermore, the monophosphate of compound A (A-P) was synthesized and evaluated for antitumor activity in Hep3B Xenograft nude mice model. The results indicated that compound A-P has excellent antitumor activity when administrated either iv or po. With excellent antitumor activity profiles, compound A-P is considered potential backup compound for CHM-l-P-Na, which is currently under preclinical study.
Relation:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
Appears in Collections:	[Pharmacy and Science] 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium

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