Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids

作     者：MENG Ying ZHANG Hongwei LIU Zehua ZENG Shanchao SUN Chiyu ZHANG Lijuan ZHAO Mingming WANG Guan JIANG Mengying SHI Wei SONG Hongrui 

作者机构：10016 P. R. China Key Laboratory for Molecular Enzymology & Engineering Ministry of Education Jilin University Changchun 130012 P. R. China 

基　　金：Supported by the Program for Liaoning Innovative Research Team in University  China 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2014年第30卷第4期

页      码：624-631页

摘      要：A series of pyrrolopyrazinone-chalcone hybrids（12a-12q） was designed,synthesized and screened for their antitumor activity against SKOV-3,A549 and HeLa cell lines in *** with the pyrrolopyrazinone（10a） and 5-fluorouracil（5-FU）,nearly all the tested compounds showed significantly-improved antitumor *** most promising compounds 12e and 12k（IC50=0.25 and 0.88 μmol/L） respectively show activities of 123and 35 times that of compound 10a（IC50=30.74 μmol/L） against HeLa cell *** result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.

主 题 词：Pyrrolopyrazinone-chalcone hybrid Antitumor Marine sponge Combination principle 

学科分类：1007[医学-药学类] 081302[081302] 08[工学] 0813[工学-化工与制药类] 10[医学] 

核心收录：

D　O　I：10.1007/s40242-014-3542-z

馆 藏 号：203735722...