Design, synthesis and antitumor activity of pyrrolopyrazinone-chalcone hybrids

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 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.

Keywords

Pyrrolopyrazinone-chalcone hybrid / Antitumor / Marine sponge / Combination principle

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