Synthesis in vitro evaluation and structure activity relationship of some heterocyclic imidazoazine derivatives

Abstract

We have synthesized various imidazo[1,2-a]pyrazine derivatives bearing aryl group at different positions and then evaluated them in vitro against cancer cell lines. Structure activity relationship predicting the relation of activity with changing substituents. As molecular hybridization is an important technique to combine two active pharmacophores in a single unit. Therefore we have applied this methodology to obtain imidazo[1,2-a]pyrazine-coumarin hybrids that have been evaluated against 60 human cancer cell lines along with prediction of SAR. The hybrids have been checked for its cytotoxicity on normal cells. More molecular conjugates/dyads have been synthesized by employing imidazo[1,2-a]pyrazine-coumarin linked to triazole and imidazo[1,2-a]pyrazine-benzimidaozle linked to triazole via click chemistry and Suzuki-Miyaura coupling reactions. Photophysical properties of all conjugates have been determined. Naphthalimide derivatives have also been synthesized which have been studied for its photophysical sensing towards various anions and metals along with DNA intercalation studies. newline