The synthesis of aryl 4‐nitro‐5‐imidazolyl sulfone radiation sensitizers sterically protected against glutathione reaction

Roger A. Egolf, Ned D. Heindel

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

2,6‐Disubstituted aryl 1‐methyl‐4‐nitro‐5‐imidazolyl sulfones 4 and aryl 1‐neopentyl‐2‐tert‐butyl‐4‐nitro‐5‐imidazolyl sulfones 10 have been synthesized and tested as radiation sensitizers of hypoxic carcinoma cells. These sterically crowded imidazoles show decreased displacement reactivity with glutathione at C‐5, a major metabolic reaction known to deplete effective plasma drug levels in traditional aryl imidazolyl sulfone radiation sensitizers.

Original languageEnglish (US)
Pages (from-to)577-582
Number of pages6
JournalJournal of Heterocyclic Chemistry
Volume28
Issue number3
DOIs
StatePublished - Jan 1 1991

All Science Journal Classification (ASJC) codes

  • Organic Chemistry

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