Potential antitumor agents. Part 29(1): synthesis and potential coanthracyclinic activity of imidazo[2,1-b]thiazole guanylhydrazones.
This paper reports the synthesis of new imidazo[2,1-b]thiazole guanylhydrazones which were tested as potential antitumor agents. Three of these derivatives (those bearing a 3- or 4-nitrophenyl group) were the most potent and one of these showed a mild effect as CDK1 inhibitor. These same three derivatives were also tested as positive inotropic agents and two of them were more potent than amrinone at 10(-5) M. These two guanylhydrazones could be useful coanthracyclinic agents.
Andreani
A
A
Dipartimento di Scienze Farmaceutiche, Università di Bologna, Italy. aldoandr@alma.unibo.it
Leoni
A
A
Locatelli
A
A
Morigi
R
R
Rambaldi
M
M
Recanatini
M
M
Garaliene
V
V
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D019791:Guanidine / Q000138:chemical synthesis / Q000494:pharmacology; D006168:Guinea Pigs; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D010210:Papillary Muscles / Q000187:drug effects; D013215:Starfish; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D006835:Hydrazones; D007093:Imidazoles; D013844:Thiazoles; D016203:CDC2 Protein Kinase; D019791:Guanidine