Tổng hợp và thử hoạt tính sinh học của một số dẫn chất benzamid có nhân quinazolin

Abstract

A series of 6 novel benzamid incorporating quinazoline heterocycles (4a-f) were synthesized as novel histone deacetylases Inhibitors. By bioevaluation, these quinazoline-based benzamide showed potent cytotoxicity against the following three human cancer cell lines: SW620 (colon), PC-3 (prostate) and NCI-H23 (lung), displaying the potency 5 - up to 10-fold higher than SAFIA (suberoylanilidehydroxamic acid, vorinostat). Also, these compounds were comparable to SAHA in inhibiting HDACs with IC₅₀ values within the sub-micromolar range. Of these, two compounds (4c) and (4f) were HDAC inhibitors even more potent than SAHA in Hela extract assay and expected to be promising anticancer drug candidates.