Biological evaluation of the 3,4-dihydro-2(1H)-quinoxalinones and 3,4-dihydro-1,4-benzoxazin-2-ones

Abstract

In order to investigate new potential therapeutically active agents, we investigated the biological properties of two small libraries of quinoxalinones and 3,4-dihydro-2(1H)-quinoxalinones (Fig. 1). The results obtained showed that compounds 5, 9–11 have good cytotoxic activity against HeLa cells where the lowest IC50 ǀalue ;ϭϬ.ϰϲ ± Ϭ.ϴϮ μM/ŵLͿ ǁas measured for compound 10. Additionally, the most active compounds (5, 9–11) showed much better selectivity for MRC-5 cells (up to 17.4) compared to cisplatin. In vitro evaluation of the iŶhiďitioŶ of the eŶzLJŵe α-glucosidase showed that compounds 10 and 11 exert significant iŶhiďitioŶ of the eŶzLJŵe at ϱϮ.ϱϰ ± Ϭ.Ϭϵ aŶd ϰϬ.Ϭϵ ± Ϭ.ϰϵ μM, ƌespeĐtiǀelLJ.