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Acetylenic antifolates as anticancer agents

Acetylenic antifolates as anticancer agents Abstract Folates are crucial cofactors involved in the de novo generation of purine and deoxythymidine monophosphate, which are essential for DNA synthesis. Antifolates are structural analogues of folate derivatives that act as inhibitors of folate-dependent enzymes and constitute the oldest antimetabolite class of anticancer agents. This review focuses on antifolates with remarkable anticancer activities that include a terminal alkyne function in their molecular structure. The properties of CB3717, a tremendous inhibitor of thymidylate synthase, are described, and the development of raltitrexed and pralatrexate, a dihydrofolate reductase inhibitor approved by the U.S. Food and Drug Administration (FDA) as the first drug for the treatment of relapsed and refractory peripheral T cell lymphoma are presented. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Pteridines de Gruyter

Acetylenic antifolates as anticancer agents

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Publisher
de Gruyter
Copyright
Copyright © 2015 by the
ISSN
0933-4807
eISSN
2195-4720
DOI
10.1515/pterid-2015-0006
Publisher site
See Article on Publisher Site

Abstract

Abstract Folates are crucial cofactors involved in the de novo generation of purine and deoxythymidine monophosphate, which are essential for DNA synthesis. Antifolates are structural analogues of folate derivatives that act as inhibitors of folate-dependent enzymes and constitute the oldest antimetabolite class of anticancer agents. This review focuses on antifolates with remarkable anticancer activities that include a terminal alkyne function in their molecular structure. The properties of CB3717, a tremendous inhibitor of thymidylate synthase, are described, and the development of raltitrexed and pralatrexate, a dihydrofolate reductase inhibitor approved by the U.S. Food and Drug Administration (FDA) as the first drug for the treatment of relapsed and refractory peripheral T cell lymphoma are presented.

Journal

Pteridinesde Gruyter

Published: Sep 1, 2015

References