Articles Accepted

In continuation with the previous work based upon pyrazoline derivatives having cytotoxic activity, twenty-one 1,3,5-substituted pyrazoline derivatives were designed taking into consideration the important functional groups of Methisazone, Sorafenib, and chalcone. The designed derivatives were screened using preliminary molecular docking simulation study for evaluation of their binding interactions with vascular endothelial growth factor receptor-2 (PDB ID: 3WZD). The synthesized derivatives were biologically evaluated for in-vivo anti-angiogenic activity using adult zebra fish, its embryo and in vitro anti-proliferative activity against pancreatic cancer MIA-PA-CA-2 cell line using the sulforhodamine B assay. In particular, compound 5b emerged as a promising hit molecule as it manifested moderate in vitro cytotoxic activity. Besides, its ability to inhibit zebra fish caudal fin regeneration with less phenotypical changes in zebra fish embryo suggests its promising potential against pancreatic cancer by VEGFR-2 inhibition as mode of action.