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SYNTHESIS OF 4-AZAPODOPHYLLOTOXINS WITH ANTICANCER ACTIVITY BY MULTICOMPONENT REACTIONS

M. G. Botes, S. C. Pelly, M. A. L. Blackie, A. Kornienko, W. A. L. van Otterlo
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Abstract


In the last 13 years, considerable advances have been made in the development of 4-azapodophyllotoxins as anticancer agents. The current review covers this research with an emphasis on the synthesis of less stereochemically complex podophyllotoxin analogs by efficient multicomponent reactions. After a short introduction to the 4-azapodophyllotoxins prepared by such reactions, the debate concerning their exact mechanisms is highlighted. This is followed by a description of 4-azapodophyllotoxin libraries and a discussion of their documented anticancer activities. The review concludes with an analysis of the proposed mode of action and future directions in this fascinating area of research.

How to Cite
Botes, M. G.; Pelly, S. C.; Blackie, M. A. L.; Kornienko, A.; van Otterlo, W. A. L. Chem. Heterocycl. Compd. 2014, 50, 119. [Khim. Geterotsikl. Soedin. 2014, 139.]

For this article in the English edition see DOI 10.1007/s10593-014-1455-x


Keywords


podophyllotoxin; 4-azapodophyllotoxins; multicomponent reaction; antiproliferative activity

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