A Dideazatetrahydrofolate Analogue Lacking a Chiral Center at C-6, N-[4-[2-(2-Amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5yl)ethyl[benzoyl]-l-glutamic Acid is an Inhibitor of Thymidylate Synthase

Edward C. Taylor, Dietmar Kuhnt, Sharon M. Rinzel, Gerald B. Grindey, Chuan Shih, Richard G. Moran, Julio Barredo, Mehrdad Jannatipour

Research output: Contribution to journalArticle

281 Scopus citations

Abstract

N- [4-[2-(2-Amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl] benzoyl]-L-glutamic acid (15), prepared in five steps from 2-pivaloyl-7-deazaguanine, has been found to be an antitumor agent with its primary site of action at thymidylate synthase rather than purine synthesis. This compound appears to be a promising candidate for clinical evaluation.

Original languageEnglish (US)
Pages (from-to)4450-4454
Number of pages5
JournalJournal of Medicinal Chemistry
Volume35
Issue number23
DOIs
StatePublished - Nov 1 1992
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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