Antitumor activity of N-heterocyclic carboxaldehyde thiosemicarbazone derivatives.
Antitumor activity of N-heterocyclic carboxaldehyde thiosemicarbazone derivatives was examined in ascites sarcoma-180 system. Among isoquinoline-1-carboxaldehyde thiosemicarbazone derivatives, the parent compound, IQ-1, was the most active and less toxic. On the other hand, 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, acetoxymethyl derivative was markedly active against Ehrlich ascites carcinoma, leukemia L-1210, and leukemia C-1498, while moderately effective against Nakahara-Fukuoka sarcoma, but it was not active against adenocarcinoma-755. Isonicotinoyl derivative was markedly active against Ehrlich ascites carcinoma, leukemia L-1210, and leukemia C-1498, while moderately active against adenocarcinoma-755, and slightly active against Nakahara-Fukuoka sarcoma.
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D005260:Female; D007942:Leukemia, Experimental / Q000188:drug therapy; D008297:Male; D051379:Mice; D012510:Sarcoma 180 / Q000188:drug therapy; D013882:Thiosemicarbazones / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D013882:Thiosemicarbazones