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Laboratory Evaluation of a New Nitrogen Mustard, 2-[Di-(2-chloroethyl)aminomethyl]benzimidazole, and of Other 2-Chloroethyl Compounds^*

( Institute of Cancer Research and Departments of Biochemistry and Medicine, Columbia University College of Physicians and Surgeons, New York 32, N.Y., and the Givaudan Corporation, Delawanna, N.J.)

A new nitrogen mustard derivative, 2-[di-(2-chloroethyl)aminomethyl]benzimidazole, in which the reactive alkylating moiety is attached to a putative purine antagonist, has been synthesized, and its carcinostatic activity against a variety of experimental mouse tumors has been evaluated. This compound inhibits not only the Ehrlich ascites carcinoma, which responds readily to many alkylating agents, but also mammary Adenocarcinomas 755 and E 0771 and Sarcoma 180. Comparative results obtained with a small series of previously known alkylating agents (antimalarial mustards, chlorambucil) and with a number of other mono- and bifunctional nitrogen mustard analogs, none of which inhibit the growth of these solid tumors significantly, are presented.

^* This investigation was supported by U.S. Public Health Service Research Grants C-1894 and C-2332, and by the Charles Ulrick and Josephine Bay Gift for Research in Chemotherapy of Brain Tumors. This material was presented in brief at the Conference on Comparative Clinical and Biological Effects of Alkylating Agents, in New York, March 28, 1957 (11), and before the American Association for Cancer Research, Chicago, April 12, 1957 (12).

Received 5/23/57.

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