Thiosemicarbazones and hydrazones of alpha-methylchalkone as potential chemotherapeutic agents.
The effectiveness of chalkones and derivatives as antibacterial and antifungal agents stimulated our interest in the possibility of coupling this type of compound with certain hydrazines and thiosemicarbazides to determine the potential chemotherapeutic activity of these combinations as anticancer and antimalarial agents. Accordingly, 18 hydrazine and thiosemicarbazide derivatives of alpha-methylchalkone (dypnone) have been synthesized for study as potential antitumor agents in animal tumor systems against Walker 256 carcinosarcoma (intramuscular) and leukemia L-1210 and for antimalarial activity against Plasmodium berghei in experimentally infected mice. Of the series of chalkone derivatives, significant inhibition in preliminary tests against the Walker 256 carcinosarcoma (intramuscular) rat tumor system was exhibited by alpha-methylchalkone-1,4-phthalazinediyldihydrazone and showed activity in the leukemia 1210 mouse tumor system. The guanylhydrazone of alpha-methylchalkone showed good inhibition with confirmed activity against Plasmodium berghei in experimentally infected mice.
D000818:Animals; D000962:Antimalarials / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D002279:Carcinoma 256, Walker / Q000188:drug therapy; D002599:Chalcone / Q000031:analogs & derivatives / Q000627:therapeutic use* / Q000633:toxicity; D002738:Chloroquine / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D006835:Hydrazones / Q000627:therapeutic use* / Q000633:toxicity; D007939:Leukemia L1210 / Q000188:drug therapy; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D008811:Mice, Inbred DBA; D010962:Plasmodium berghei; D011427:Propiophenones / Q000627:therapeutic use*; D013882:Thiosemicarbazones / Q000627:therapeutic use* / Q000633:toxicity
D000962:Antimalarials; D000970:Antineoplastic Agents; D006835:Hydrazones; D011427:Propiophenones; D013882:Thiosemicarbazones; D002599:Chalcone; D002738:Chloroquine