synthesis and biological evaluation of new 5-fluorouracil-substituted ampelopsin derivatives合成和生物评价的新5-fluorouracil-substituted ampelopsin衍生品.pdf

Molecules 2010, 15, 2114-2123; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Biological Evaluation of New 5-Fluorouracil- Substituted Ampelopsin Derivatives Wei-Ming Zhou 1,2,†, Rong-Rong He 1,†, Jian-Tao Ye 1, Na Zhang 1 and De-Yu Liu 1,* 1 School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China; E-Mails: weiming81@126.com (W.-M.Z.); herongrong22@163.com (R.-R.H.); yejt@ (J.-T.Y.); nanon120@ (N.Z.) 2 Guangdong Food and Drug Vocational College, Guangzhou 510520, China; † These authors contributed equally to this work. * Author to whom correspondence should be addressed; E-Mail: liudeyu@. Received: 19 January 2010; in revised form: 15 March 2010 / Accepted: 22 March 2010 / Published: 24 March 2010 Abstract: This study reports two novel 5-fluorouracil-substituted ampelopsin derivatives. The structures of two new derivatives were characterized by elemental analysis, 1H-NMR, 13C-NMR, IR and MS. Their anticancer activities in vitro against two cancer cell lines, K562 and K562/ADR, were investigated using the MTT assay, and the results showed that the two new compounds were more effective than reference drugs such as ampelopsin and verapamil. Keywords: ampelopsin; 5-fluorouracil; anticancer activity 1. Introduction Ampelopsin (3,5,7,3′,4′,5′-hexahydroxyl-2,3-dihydroflavonol, CAS: 27200-12-0, 1) is a purified component of the tender stems and leaves or roots of the Chinese medicinal herbs