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 

机构地区：[1]Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang ]10016, P. R. China [2]Key Laboratory for Molecular Enzymology & Engineering, Ministry of Education, Jilin University, Changchun 130012, P. R. China

出　　处：《Chemical Research in Chinese Universities》2014年第4期624-631,共8页高等学校化学研究（英文版）

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 vitro.Compared with the pyrrolopyrazinone（10a） and 5-fluorouracil（5-FU）,nearly all the tested compounds showed significantly-improved antitumor activities.The 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 line.The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.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 vitro.Compared with the pyrrolopyrazinone（10a） and 5-fluorouracil（5-FU）,nearly all the tested compounds showed significantly-improved antitumor activities.The 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 line.The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.

关 键 词：Pyrrolopyrazinone-chalcone hybrid ANTITUMOR Marine sponge Combination principle 

分 类 号：TQ463.5[化学工程—制药化工] TU201.1[建筑科学—建筑设计及理论]