synthesis and in vitro protein tyrosine kinase inhibitory activity of furan-2-yl(phenyl)methanone derivatives合成和体外蛋白质酪氨酸激酶抑制活性furan-2-yl(苯)methanone衍生品.pdf

Molecules 2011, 16, 4897-4911; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and In Vitro Protein Tyrosine Kinase Inhibitory Activity of Furan-2-yl(phenyl)methanone Derivatives 1 1 1 1 2 Fei Lang Zheng , Shu Rong Ban , Xiu E Feng , Cheng Xiao Zhao , Wenhan Lin and Qing Shan Li 1,2,* 1 School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, Shanxi, China 2 State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China * Author to whom correspondence should be addressed; E-Mail:qingshanl@; Tel.: +86-351-4690322; Fax: +86-351-4690114. Received: 27 April 2011; in revised form: 1 June 2011 / Accepted: 7 June 2011 / Published: 14 June 2011 Abstract: A series of novel furan-2-yl(phenyl)methanone derivatives were synthesized, and their structures were established on the basis of 1H-NMR, 13C-NMR and mass spectral data. All the prepared compounds were screened for their in vitro protein tyrosine kinase inhibitory activity and several new derivatives exhibited promising activity, which, in some cases, was identical to, or even better than that of genistein, a positive reference compound. The preliminary structure-activity relationships of these compounds were investigated and are discussed. Keywords: halophenols; furan-2-yl(phenyl)methanone; protein tyrosine kinases inhibitor; structure-activ