Rational design, molecular docking and synthesis of novel homopiperazine linked imidazo[1,2-alpha]pyrimidine derivatives as potent cytotoxic and antimicrobial agents

摘要

Designed and synthesized novel homopiperazine linked imidazo [1,2-alpha] pyrimidine derivatives (10a-i, 11a-g, 12), and evaluated them for their in vitro cytotoxicity against HeLa cells (cervical cancer), A549 cells (lung cancer) cells, by MTT assay. Compound 12 (IC50, = 4.14 mu M) and compound 10c (IC50 = 5.98 mu M) were found to be 2.5 fold, and 1.74 fold more potent when compared with standard Etoposide (IC50 = 10.44 mu M), against A549 (lung cancer cells). Compound 12 also found to be 1.57 and 1.13 fold potent against DU145 (IC50 = 6.24 mu M) and HeLa (IC50, = 6.54 mu M), respectively when compared with Etoposide (DU145, IC50 = 9.8 mu M; HeLa, IC50, = 7.43 mu M). Compound 10f (IC50, = 6.12 mu M) was found to be 1.31 fold more potent than Etoposide (IC50 = 7.43 mu M) against HeLa cell lines.