Articles

Investigations into the Lymphopaenic and lmmunosuppressive Properties of the Antitumour Agent, Mitoclomine

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Abstract

The formula of Mitoclomine (W.B. 7007) was suggested by Granger in 1966 (1) as that of a useful cytotoxic agent, and confirmed in a number of experimental tumours.

It had been shown previously that the synthetic vitamin K, Synkavit was concentrated by some tumour systems (2, 3) arid possessed useful radiosensitising properties (4, 5). Vitamin K5, although not studied to the same extent as Synkavit, was also thought to share those properties and the molecule lent itself to substitution of the amine radicle with a N-N-bischlorethyl group.

Previous studies by Whisson and Connors (6, 7) had demonstrated that in aniline mustard compounds the group in the para position to a mustard on the benzene ring could influence the overall toxicity and cytotoxic activity of the compound. A parahydroxy aniline mustard derivate had increased toxicity and decreased therapeutic index when compared with aniline mustard itself, but a paramethoxy derivative showed an increased cytotoxic activity with decreased toxicity. The vitamin K5 molecule was, therefore, modified further by substituting a methoxy for a hydroxy group. Granger (1) reported that this compound possessed useful cytotoxic activity against various animal tumour systems. An additional observation was that of a concurrent selective depressant effect on the blood lymphocyte without reduction of the polymorphonuclear count.

How to Cite:

Fox, M., Rees, R., Bennett, D. & Henry, L., (1971) “Investigations into the Lymphopaenic and lmmunosuppressive Properties of the Antitumour Agent, Mitoclomine”, Lymphology 4(2), 35-47.