Synthesis and Evaluation of Cytotoxic Activity of 2-Aryl-2-(3-Indolyl)Propionic Acid Derivatives

Abstract

2-Aryl-2-(3-indolyl)acetohydroxamic acids have emerged as promising antitumor agents; however, their poor pharmacokinetic profile remains a significant drawback. To address this limitation, we have synthesized a homolog of such acids—specifically 2-aryl-2-(3-indolyl)propionic acid (IC50 > 100 mM (U87)), along with several other derivatives: ethyl ester (IC50 > 100 mM (U87)), hydroxamate (IC50 21.2 ± 1.0 mM (U87)) and hydrazide (IC50 > 100 mM (U87)). The cytotoxicity of these compounds against glioblastoma cell lines was evaluated and compared to that of the parent acetohydroxamic acid derivatives.