One‐Pot Synthesis of Some New Isatin‐1,2,4‐oxadiazole Hybrids as VEGFR‐2 Aiming Anticancer Agents
Sunitha Boda, Satheesh Kumar Nukala, Ravinder Manchal
Abstract
Abstract The one‐pot synthesis of some new isatin‐1,2,4‐oxadiazole hybrids ( 3 a – n ) in moderate to good yields via reaction between 3‐((1‐methyl‐2‐oxoindolin‐3‐ylidene)amino)propane nitrile and several aromatic carboxylic acids using the key reagents like NH 2 OH.HCl, Et 3 N and POCl 3 /DMF was described herein. The synthesized compounds were screened for the cytotoxicity against three human cancer cell lines such as A549, PC3, DU145 and MCF7. Among them, three compounds ( 3 d , 3 e and 3 l ) were exhibited superior activity than the standard 5‐fluorouracil against all the cell lines. In vitro VGEFR‐2 tyrosine kinase assay on 3 d , 3 e and 3 l indicates that 3 l has more inhibiting power than the standard sorafenib.Further, in silico studies like molecular docking studies on VEGFRs and ADMET performed to know binding affinity towards VEGFRs and drug likeness properties.