Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids

doi:10.1007/s40242-014-3542-z

Abstract

Abstract:

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 acti- vities. 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.

Key words: Pyrrolopyrazinone-chalcone hybrid, Antitumor, Marine sponge, Combination principle

MENG Ying, ZHANG Hongwei, LIU Zehua, ZENG Shanchao, ZHANG Hongwei, SUN Chiyu, ZHANG Lijuan, ZHAO Mingming, WANG Guan, JIANG Mengying, SHI Wei, SONG Hongrui. Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids[J]. Chemical Research in Chinese Universities, 2014, 30(4): 624-631.

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