IsatinAs AScaffold For Anticancer Drug Development,Mechanistic Insights, And Therapeutic Applications

Isatin derivatives have received considerable attention in recent years as potential anticancer agents because of their potential to modulate several molecular targets implicated in cancer cell propagation. The present systematic review analyzes articles published from 2011-2020, which focused on the findings of the anticancer effects of isatin derivatives. 180 articles were identified from electronic databases and other sources before the records were further screened according to the selection criteria. The current study involved a total of 20 samples for both qualitative and quantitative analyses. From the foregoing discussions, the principal anticancer processes of isatin derivatives include apoptotic, cell cycle, DNA, ROS, and autophagy activities. 5-Fluoroisatin emerges as a highly potent apoptotic inducer via caspase-3 activation in both MCF-7 and A549 cell lines (IC50 = 2.5 µM). Mitochondria were targeted in HepG2 and HeLa cells with Isatinoxime with an IC50 of 3.1 µM for disruption of the mitochondrial membranes, N-Methyl-isatin bound DNA, specifically in prostate cancer cells with an IC of 1.8 µM. Other derivatives the Isatinthiosemicarbazone, caused the formation of ROS, while Halogenated isatin affected topoisomerase II activity in leukemia cells. Isatin conjugated with peptide moiety was found to inhibit both EGFR and VEGFR signaling pathways in cancer cells of liver and lung cancers.