Key structural requirements of benzamide derivatives for histone deacetylase inhibition: design, synthesis and biological evaluation.

ABSTRACT: Background: Histone deacetylase inhibitors (HDACIs) are important as anticancer agents. Objective: This study aimed to investigate some key structural features of HDACIs via the design, synthesis and biological evaluation of novel benzamide-based derivatives. Methods: Novel structures, designed using a molecular modification approach, were synthesized and biologically evaluated. Results: The results indicated that a subset of molecules with CH₃/NH₂ at R₂ position possess selective antiproliferative activity. However, only those with an NH₂ group showed HDACI activity. Importantly, the shorter the molecule length, the stronger HDACI. Among all, 7j was the most potent HDAC1-3 inhibitor and antiproliferative compou

SUBMITTER: Cheshmazar N 

PROVIDER: S-EPMC11188831 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature