ANTITUMOR ACTIVITY OF N-HETEROCYCLIC CARBOXALDEHYDE THIOSEMICARBAZONE DERIVATIVES

  • 1 January 1977
    • journal article
    • research article
    • Vol. 68  (2) , 221-225
Abstract
Antitumor activity of N-heterocyclic carboxaldehyde thiosemicarbazone derivatives was examined in mouse ascites sarcoma 180. Among isoquinoline-1-carboxaldehyde thiosemicarbazone derivatives, the parent compound, IQ-1, was the most active and less toxic. Among the pyridine-2-carboxaldehyde thiosemicarbazone derivatives tested, 5-acetoxymethyl and 5-isonicotinoyl derivatives were active, and their therapeutic indices were 190 and 54, respectively. In other tumor systems, the acetoxymethyl derivative was active against Ehrlich ascites carcinoma, leukemia L-1210 and leukemia C-1498, while it was moderately effective against Nakahara-Fukuoka sarcoma, and inactive against adenocarcinoma 755. The isonicotinoyl derivative was active against Ehrlich ascites carcinoma, leukemia L-1210 and leukemia C-1498, while it was moderately active against adenocarcinoma 755, and slightly active against Nakahara-Fukuoka sarcoma.

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