synthesis and biological evaluation of 7-o-modified formononetin derivatives合成和生物评价7-o-modified芒柄花黄素衍生品.pdfVIP

Hindawi Publishing Corporation Research Letters in Organic Chemistry Volume 2008, Article ID 209830, 4 pages doi:10.1155/2008/209830 Research Letter Synthesis and Biological Evaluation of 7-O-Modified Formononetin Derivatives Ying Yang, Wen-Jun Mao, Huan-Qiu Li, Tao-Tao Zhu, Lei Shi, Peng-Cheng Lv, and Hai-Liang Zhu School of Life Sciences, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China Correspondence should be addressed to Hai-Liang Zhu, zhuhl@ Received 15 July 2008; Accepted 27 September 2008 Recommended by Alexander Greer Three series of novel formononetin derivatives were synthesized, in which formononetin and heterocyclic moieties were separated by 2-carbon, 3-carbon, and 4-carbon spacers. The chemical structures of these compounds were confirmed. All the derivatives were screened for antiproliferative activities against Jurkat cell line and HepG-2 cell line. In this paper, compounds prepared were also screened for their antibacterial activity of six bacterial strains. Compound 3b exihibited promising antibacterial activity against B. subtilis with minimal inhibitory concentration (MIC) value of 0.78 μg/mL, and compound 5e showed significant antiproliferative activities against Jurkat cell growth with IC50 of 1.35 × 10−4 μg/mL. The preliminary investigation of structure-activity relationships (SARs) was also discussed based on the obtained experimental data. Copyright © 2008 Ying Yang et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. 1. Introduction [10– 14]. Formononetin is also a potent aryl h