Synthesis and In Vitro Evaluation of Heterocyclic Core Moieties as Anticancer Agents

Abstract

In present investigation, we have synthesized benzimidazole bearing naphthalimide analogues as well as N-allyl naphthalimides. These analogues were substituted with variety of primary and secondary amines. Keeping in mind, their DNA intercalating properties, UVVisible and fluorescence spectrophotometry and thermal denaturation experiments were performed with the most active compounds. Similarly, 2,3-disubstituted pyridine analogue appended 1,2,3-triazole motifs were synthesized. Characterization of these molecules was done with different spectroscopic techniques such as 1H NMR, 13C NMR and mass 126 spectroscopy. The synthesized molecules were evaluated in vitro over 60 human cancer cell lines. ct-DNA studies have been done for finding the probable interaction with DNA. Structure-activity relationship studies were used to identify the structural features of these novel compounds. In order to have an insight into the molecular interactions of these compounds, their docking were also planned to scrutinize the mode of interaction of compound with amino acids in the active site of the enzyme.