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The Antitumor Activity of Cu(II)KTS, the Copper(II) Chelate of 3-Ethoxy-2-oxobutyraldehyde Bis(thiosemicarbazone)

Biochemical Research Division, The Upjohn Company, Kalamazoo, Michigan

The antitumor activity of the copper(II) chelate of 3-ethoxy-2-oxobutyraldehyde bis(thiosemicarbazone), Cu(II)KTS, against the Walker 256 carcinosarcoma in rats is shown, and the importance of considering this chelate as the active intermediate in the mechanism of action of the free ligand, KTS, is indicated. The potentiation of the antitumor activity and toxicity of Cu(II)KTS by KTS and Vu(II) was demonstrated. Results of experiments with combinations of these agents are consistent with the hypothesis that the dynamics of the chemical equilibria governing the interaction of KTS and Cu(II) to form Cu(II)KTS also govern their biologic activity. The protonated chelate, Cu(II)KTS·2HCl, appears to be less active as an antitumor agent than is the uncharged chelate but also somewhat more toxic for rats.

¹ Present address: Kettering Laboratory, College of Medicine, University of Cincinnati, Cincinnati, Ohio. This address should be used in all correspondence.

Received 9/30/66. Accepted 3/27/67.

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