Advances in Anticancer Agents in Medicinal Chemistry

Volume: 2

Indexed in: Book Citation Index, Science Edition, EBSCO, Ulrich's Periodicals Directory

Advances in Anticancer Agents in Medicinal Chemistry is an exciting eBook series comprising a selection of updated articles previously published in the peer-reviewed journal Anti-Cancer Agents in ...
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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


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.


Isatin, indolinone, cytotoxicity, anticancer, kinase, drug conjugates, enzyme inhibitor, structure-activity relationships.


Illawarra Health and Medical Research Institute, University of Wollongong, Wollongong, NSW, 2522, Australia