Design, synthesis and antitumor activity of pyrrolopyrazinone-chalcone hybrids
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- 作者：Ying Meng (1)
Hongwei Zhang (1)
Zehua Liu (1)
Shanchao Zeng (1)
Hongwei Zhang (1)
Chiyu Sun (1)
Lijuan Zhang (1)
Mingming Zhao (1)
Guan Wang (2)
Mengying Jiang (2)
Wei Shi (2)
Hongrui Song (1) - 关键词：Pyrrolopyrazinone ; chalcone hybrid ; Antitumor ; Marine sponge ; Combination principle
- 刊名：Chemical Research in Chinese Universities
- 出版年：2014
- 出版时间：August 2014
- 年：2014
- 卷：30
- 期：4
- 页码：624-631
- 全文大小：510 KB
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21. Lv Z. L., Gao Y., Li J., Huang T.K., He S. J., Zou Y., / Chem. J. Chinese Universities, 2013, / 34(11), 2531 - 作者单位：Ying Meng (1)
Hongwei Zhang (1)
Zehua Liu (1)
Shanchao Zeng (1)
Hongwei Zhang (1)
Chiyu Sun (1)
Lijuan Zhang (1)
Mingming Zhao (1)
Guan Wang (2)
Mengying Jiang (2)
Wei Shi (2)
Hongrui Song (1)
1. Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, P. R. China
2. Key Laboratory for Molecular Enzymology & Engineering, Ministry of Education, Jilin University, Changchun, 130012, P. R. China - ISSN：2210-3171
文摘
A series of pyrrolopyrazinone-chalcone hybrids(12a-strong class="a-plus-plus">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 123 and 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.