Novel antitumor 2-cyanoaziridine-1-carboxamides.
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.
Iyengar
B S
BS
Department of Pharmacology and Toxicology and Arizona Cancer Center, University of Arizona, Tucson 85721, USA.
Dorr
R T
RT
Alberts
D S
DS
Hersh
E M
EM
Salmon
S E
SE
Remers
W A
WA
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001388:Aziridines / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured