Novel quinazoline-triazole-based <i>N</i>-hydroxybenzamides/<i>N</i>-hydroxypropenamides as HDAC inhibitors: design, synthesis, biological evaluation, and docking studies.

ABSTRACT: Herein, two novel series of N-hydroxybenzamides and N-hydroxypropenamides incorporating 4-oxoquinazoline and 1,2,3-triazole scaffolds were rationally designed, synthesized, and evaluated for their Histone deacetylase (HDAC) inhibitory and anticancer activities. The synthesized hydroxamic acids were evaluated for HDAC inhibitory activity using nuclear extracts from HeLa cells. N-hydroxybenzamide derivatives (7a-i) exhibited stronger HDAC inhibition than their N-hydroxypropenamide counterparts (11a-i). Compounds 7h (7-Br) and 7c (7-CH₃) were the most potent inhibitors, with IC₅₀ values of 0.142 and 0.146 μM, respectively, which are comparable to that of the positive control, SAHA. Structural modifications at positions 6 and 7 of the quinazoli

SUBMITTER: Dung NP 

PROVIDER: S-EPMC12282580 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature