Novel antitumor 2-cyanoaziridine-1-carboxamides

  • J Med Chem. 1999 Feb 11;42(3):510-4. doi: 10.1021/jm980600x.
B S Iyengar  1 ,  R T Dorr ,  D S Alberts ,  E M Hersh ,  S E Salmon ,  W A Remers
Affiliations
  • 1. Department of Pharmacology and Toxicology and Arizona Cancer Center, University of Arizona, Tucson 85721, USA.
PMID: 9986721 DOI: 10.1021/jm980600x
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.

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