Novel antitumor 2-cyanoaziridine-1-carboxamides

Bhashyam S. Iyengar, Robert T. Dorr, David S. Alberts, Evan M. Hersh, Sydney E. Salmon, William A. Remers

Research output: Contribution to journalArticle

17 Scopus citations

Abstract

A set of 20 2-cyanoaziridine-1-carboxamides was synthesized from 2- cyanoaziridine and appropriate isocyanates. These compounds were active against a variety of solid and hematological tumor cells in culture, including strains resistant to doxorubicin and mitoxantrone. Their potencies in these assays correlated with the lipophilicity of substituents. The N- phenyl derivative was more potent and equally effective to imexon, a cyclized 2-cyanoaziridine-1-carboxamide of clinical interest, against cloned fresh human tumors.

Original languageEnglish (US)
Pages (from-to)510-514
Number of pages5
JournalJournal of Medicinal Chemistry
Volume42
Issue number3
DOIs
StatePublished - Feb 24 1999

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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