Studies on the mechanism of action of the tumour inhibitory triazenes

doi:10.1016/0006-2952(73)90045-2

Biochemical Pharmacology

Volume 22, Issue 15, 1 August 1973, Pages 1855-1860, IN1-IN2, 1861-1864

https://doi.org/10.1016/0006-2952(73)90045-2 Get rights and content

Abstract

A series of imidazole and phenyl dialkyi triazenes were synthesized and investigated for their anti-cancer activity in experimental animals. Active triazenes had a broad spectrum of anti-tumour action and like bischloroethylnitrosourea (BCNU) were active against tumours not sensitive to conventional alkylating agents. It was confirmed that at least one N-methyl group was necessary for anti-cancer activity but there was no correlation between dealkylation by liver microsomes and activity since a diethyl triazene was readily dealkylated but not active. A factor appears to be present in normal cell cytoplasm which can detoxify triazenes but which is absent from tumours sensitive to these agents.

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^∗: Present address: Faculty of Pharmacy, University of Manitoba, Winnipeg, Manitoba, Canada.

^‡: Present address: George Washington University, School of Medicine, Washington, D.C., U.S.A.

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Studies on the mechanism of action of the tumour inhibitory triazenes

Abstract

Biochem. Pharmac

Eur. J. Cancer.

Biochem. Pharmac.

Toxic. Appl. Pharmac.

Biochem. Pharmac.

J. biol. Chem.

Archs Biochem. Biophys.

J. biol. Chem.

Eur. J. Cancer

Biochem. Pharmac.

J. med. Chem.