Work

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

Year: 2025

Type: article

Abstract: -hydroxypropenamide derivatives generally had stronger antiproliferative effects. The 6-Cl derivatives (7d, 11d) exhibited the highest cytotoxic activity, highlighting the significance of halogen substitution. Selectivity assessments against normal human lung fibroblasts (MRC-5) indicated that most compounds were more toxic to cancer cells. Notably, 7d and 11d induced G2/M phase arrest and apoptosis, demonstrating their potential as HDAC inhibitors with promising anticancer properties. Finally, molecular docking studies on HDAC isoforms for the 7a-i and 11a-i series revealed key structural features crucial for the activity of the library compounds.

Source: RSC Advances

DOI: 10.1039/d5ra04193g