Synthesis and Biological Evaluation of 2,5-Diaminobenzamide Derivatives as Anti-proliferating Agents

Abstract

The screening of the chemical library for the anti-proliferative activity of the chemical library provided 2,5-diaminobenzamide as the initial hit. The confirmation and the optimization of hit were performed by synthesis followed by the evaluation of growth inhibitory activity against human cancer cell lines. The most active growth inhibitor showed IC50 of 1.0 μM. The compound 7 increased not only sub-G1 population but also number of cells which are stained with Annexin V-FITC and 7-AAD, suggesting that compound 7 induced cell death is apoptosis.

Key words Anti-cancer agent – 2,5-Diaminobenzamide – Growth inhibitory activity – Apoptosis