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The Carcinostatic Activity of -(N) Heterocyclic Carboxaldehyde Thiosemicarbazones

I. Isoquinoline-1-carboxaldehyde Thiosemicarbazone¹

Cancer Chemotherapy Research Department, Mount Zion Hospital and Medical Center, San Francisco, California

Isoquinoline-1-carboxaldehyde thiosemicarbazone (IQ-1) has been shown to have carcinostatic activity against leukemias L-1210 and ML-1210, the Lewis lung carcinoma, Adenocarcinoma 755, and the Ehrlich ascites carcinoma. IQ-1² is active, in some instances, by both oral and parenteral routes and with delayed treatment. This compound is a member of a broad class of -(N) heterocyclic carboxaldehyde thiosemicarbazones, several of which have demonstrable carcinostatic activity. The common feature of these compounds is that they contain an N*—N*—S* tridentate ligand system.

¹ This work was supported by Grant CA-03287 from the National Cancer Institute. A preliminary account appeared in Proc. Am. Assoc. Cancer Res., 6: 20, 1965.

² The abbreviations used are: IQ-1, isoquinoline-1-carboxaldehyde thiosemicarbazone; LD₅₀, median lethal dose; LLC, Lewis lung carcinoma; KTS, 3-ethoxy-2-ketobutyraldehyde bis(thiosemicarbazone).

Received 12/ 8/64. Revised 5/10/65.