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 Citations (Scopus)

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 - 1999

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Tumors
Isocyanates
Mitoxantrone
Cell culture
Doxorubicin
Assays
Neoplasms
Cell Culture Techniques
Cells
Derivatives
4-imino-1,3-diazabicyclo(3.1.0)hexan-2-one

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Novel antitumor 2-cyanoaziridine-1-carboxamides. / Iyengar, Bhashyam S.; Dorr, Robert T; Alberts, David S; Hersh, Evan M; Salmon, Sydney E.; Remers, William A.

In: Journal of Medicinal Chemistry, Vol. 42, No. 3, 1999, p. 510-514.

Research output: Contribution to journalArticle

Iyengar, Bhashyam S. ; Dorr, Robert T ; Alberts, David S ; Hersh, Evan M ; Salmon, Sydney E. ; Remers, William A. / Novel antitumor 2-cyanoaziridine-1-carboxamides. In: Journal of Medicinal Chemistry. 1999 ; Vol. 42, No. 3. pp. 510-514.
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