Pyrrole indolin-2-One Based Kinase Inhibitor as Anti-Cancer Agents

Abstract

Cancer cells are characterized by uncontrolled proliferation after escaping from inherent physiological constraints on growth and survival and by destructive invasion of the healthy surrounding tissues. Many kinases involved in signal transduction are overactive in malignant tumor cells. Thus, pharmacotherapeutic interventions targeting kinases responsible for signal transduction of cancer hallmarks have become promising in developing novel anticancer agents. Pyrrole indolin-2-one (or pyrrole oxindole, 1), a lead scaffold of kinase inhibitors, is used for anti-angiogenesis via inhibiting vascular endothelial growth factor receptors (VEGFs) and platelet-derived growth factor receptors (PDGFRs). The kinase selectivity and inhibitory activity of pyrrole indolin-2-one 1 can be significantly influenced through structural modifications. This mini-review provides a detailed overview of structural modification of pyrrole indolin-2-one derivatives for the development of novel kinase inhibitors.