[Carbonyl derivatives of tilorone. Part 2: On the cancerostatic activity of carbonyl derivatives of tilorone (author's transl)].
A series of carbonyl derivatives of tilorone was synthetized by reaction with appropriate amino compounds, mainly hydrazines and hydrazides. The condensation products obtained were tested for cancerostatic activity against the murine leucaemia L 1210 and the Walker carcinosarcoma of the rat. Only three of the substances under investigation (1a, 5, 13) proved active against the Walker carcinosarcoma, one of which (5) being comparable to tilorone. No activity against L 1210 was observed, even tilorone exerted no effect. The reduction in activity against the Walker carcinosarcoma which resulted from the carbonyl substitution might be caused by a decrease in the ability to intercalate into DNA.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002279:Carcinoma 256, Walker / Q000188:drug therapy; D005449:Fluorenes / Q000494:pharmacology*; D006834:Hydrazines / Q000138:chemical synthesis / Q000494:pharmacology; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D051381:Rats; D013994:Tilorone / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*
D000970:Antineoplastic Agents; D005449:Fluorenes; D006834:Hydrazines; D013994:Tilorone
Carbonylderivate des Tilorons. 2. Mitteilung: Zur cancerostatischen Wirksamkeit von Carbonylderivaten des Tilorons.