Recent Highlights in the Development of Isatin-Based Anticancer Agents
Pp. 254-312 (59)
Kara L. Vine, Lidia Matesic, Julie M. Locke and Danielle Skropeta
Abstract
Isatin (1H-indole-2,3-dione) and its derivatives are responsible for a broad
spectrum of biological activities. Among these the cytotoxic and antineoplastic
properties have been the most widely reported. The synthetic versatility of the isatin,
due to its privileged scaffold, has led to the generation of a large number of structurally
diverse derivatives which include analogues derived from either mono-, di-, and trisubstitution
of the aryl ring A, and/or those obtained by derivatisation of the isatin
nitrogen and C2/C3 carbonyl moieties. These compounds inhibit cancer cell
proliferation and tumour growth via interaction with a variety of intracellular targets
such as DNA, telomerase, tubulin, P-glycoprotein, protein kinases and phosphatases.
Herein we review recent highlights in the development of isatin-based compounds as
anticancer agents with a particular focus on the cytotoxicity and structure activity
relationships.
Keywords:
Isatin, indolinone, cytotoxicity, anticancer, kinase, drug conjugates,
enzyme inhibitor, structure-activity relationships.
Affiliation:
Illawarra Health and Medical Research Institute, University of Wollongong, Wollongong, NSW, 2522, Australia