Synthesis and Biological Evaluation of Novel Triazolyl-Acridine Derivatives as Cytotoxic Agents

Abstract

Novel triazolyl-acridine compounds were synthesized in 4 series of 9-(2-(substituted phenyl-1H-1,2,3-triazol-1-yl)ethoxy)acridine, 9-(3-(4-(2-substituted phenyl)-1H-1,2,3-triazol-1-yl)propoxy) acridine, N-(2-(4 substituted phenyl-1H-1,2,3-triazol-1-yl)ethyl)acridin-9-amine and N-(3-(4-(substituted phenyl)-1H-1,2,3-triazol-1-yl)propyl)acridin-9-amine using appropriate synthetic procedures and screened for cytotoxic activity. The structures of all synthesized compounds were confirmed by Fourier-transform infrared spectroscopy, proton nuclear magnetic resonance and mass spectroscopy and these compounds were assayed in vitro for cytotoxic activity against MCF-7 (human breast adenocarcinoma cell line) and HT-29 (human colon adenocarcinoma cell line) cells. Tested compounds showed better cytotoxic activities in terms of IC50 value against MCF-7 and HT-29 cells. Methyl substituted compound MPP-9 exhibited excellent sensitivity with IC50 value 1 and 2 µM, against MCF-7 and HT-29, respectively. Unsubstituted MPP-1 and chloro-substituted MPP-2 and MPP-5 also exhibited good IC50 value ranges from 2-4 µM against both cell lines. These compounds were active at micro molar concentrations. Data study revealed that synthesized compounds are promising leads for future as cytotoxic agents.