Tổng hợp và thử hoạt tính sinh học của một số dẫn chất A-hydroxyhenzamid mới mang khung 2-methylquinazolin-4(3H)-on

Abstract

Four novel N-hydroxybenzamides incorporating 2-methylquinazolin-4(3H)-one were synthesized and evaluated for cytotoxicity against the 3 folloing human cancer cell lines: SW620 (colon), PC-3 (prostate) and NCI-H23 (iung). These compounds were obtained in good yield from corresponding 2-aminobenzoic acids via a four-step synthetic pathway. These synthesized compounds all four showed strong cytotoxicity against the 3 tested cell lines with IC5G values of 0.46-3.88 mM, matchable or even stronger than SAHA (ICsg values of 2.80-3.14 mM, a positive control). Also, by Hela cell nuclear extract assay, the synthesized compounds exhibited strong HDAC inhibition with ICV values of 0.62-1.190 mM.