PMID: 3761307Oct 1, 1986Paper

Preparation and antitumor activity of 7-substituted 1,2-aziridinomitosenes

Journal of Medicinal Chemistry
B S IyengarW T Bradner

Abstract

7-Methoxy-1,2-aziridinomitosenes were prepared from mitomycin A and its N-methyl homologue by catalytic reduction followed by air oxidation. Treatment of these products with amines, including ammonia, ethylenimine, 2-methylethylenimine, propargylamine, and furfurylamine gave the corresponding 7-(substituted amino) derivatives. Screening of these compounds against P-388 leukemia in mice revealed some good activities. The more easily reduced compounds gave prolongation of life span comparable to that of mitomycin C, but their optimal doses were higher. Among these compounds, a methyl group on the aziridine nitrogen increased potency. The 7-amino derivatives, which were difficult to reduce to hydroquinones, were essentially inactive. The aziridinomitosenes were subjected to a Hansch-type analysis, but no statistically significant correlation was found.

Citations

Dec 1, 1990·Journal of Pharmaceutical Sciences·A TalebianP S Schein
Apr 29, 2021·Chemical Communications : Chem Comm·Thomas Varlet, Géraldine Masson
May 7, 2021·Organic Letters·Xinwei HuWei Zeng
Jun 2, 2021·Organic & Biomolecular Chemistry·Guang-Xin RuGuang-Qin Gao
Dec 18, 2003·Journal of the American Chemical Society·Edwin VedejsHarold Kohn

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