title: Novel antitumor 2-cyanoaziridine-1-carboxamides.
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.
authors.affiliation: Department of Pharmacology and Toxicology and Arizona Cancer Center, University of Arizona, Tucson 85721, USA.
authors.forename: B S
authors.initials: BS
authors.lastname: Iyengar
authors.forename: R T
authors.initials: RT
authors.lastname: Dorr
authors.forename: D S
authors.initials: DS
authors.lastname: Alberts
authors.forename: E M
authors.initials: EM
authors.lastname: Hersh
authors.forename: S E
authors.initials: SE
authors.lastname: Salmon
authors.forename: W A
authors.initials: WA
authors.lastname: Remers
mesh_terms: 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