Synthesis, Evaluation and Docking Studies of Disubstituted N‐Heterocyclic Derivatives as Anticancer Agents

Abstract

Cancer is a chronic disease reported with alarming rates of mortalities every year. Herein, we reported the synthesis of nitrogen based novel heterocyclic disubstituted derivatives and evaluated them against L929 and A549 cell lines using MTT assay. Among all, 6a2 and 6c1 were significantly active against L929 with IC50 value of 2.61±9.58 and 2.64±8.97 µg/mL respectively. Compounds 6a2 and 6c1 were also active against A549 with IC50 value of 2.36±9.20 and 2.43±6.28 µg/mL respectively and were found to be more potent than the standard drug Doxorubicin. A molecular docking study of the active compounds was also done against EGFR, conferring good binding affinity and binding interactions. Further biological investigations may provide valuable insights towards exploring the therapeutic potential of the active compounds in future.