5′-Halogenated formycins as inhibitors of 5′-deoxy-5′-methylthioadenosine phosphorylase: Protection of cells against the growth-inhibitory activity of 5′-halogenated adenosines

Shih Hsi Chu, Lynn Ho, Edward Chu, Todd Savarese, Zhi Hao Chen, Elizabeth Claflin Rowe, Ming Yu Wang Chu

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

A series of 5′-halogenated formycins, including the chloro-, bromo- and iodo- derivatives, were synthesized. These compounds are competitive inhibitors of 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAPase) with Ki values in the range of 10−7 M, making them the most potent inhibitors of MTAPase reported to date. These compounds protect cells from the growth-inhibitory action of 5′-halogenated adenosines, which must be activated by MTAPase. The syntheses of 5′-halogenated formycin B derivatives, which inhibit purine nucleoside phosphorylase, are also described.

Original languageEnglish (US)
Pages (from-to)185-200
Number of pages16
JournalNucleosides and Nucleotides
Volume5
Issue number2
DOIs
StatePublished - May 1 1986
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Genetics

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