Synthesis and antitumor activity of hydrosoluble analogs of p-(3,3-dimethyl-1-triazeno) benzoic acid potassium salt.
The hydrosoluble triazene derivatives of phenylacetic, phenylbutyric and cinnamic acid have been synthesized and their logP and pKa values were simultaneously determined according to a multiparametric fitting of potentiometric data. The antitumor activity caused by the synthesized compounds in mice bearing either Lewis lung carcinoma or TLX5 lymphoma was evaluated and discussed in comparison with the parent compound (p-(3,3-dimethyl-1-triazeno)benzoic acid potassium salt (DM-COOK, CAS 70055-49-1). The tested compounds were at least as active as DM-COOK, the cinnamic and the phenylacetic derivatives being the more active compounds in mice bearing TLX5 lymphoma and Lewis lung carcinoma, respectively.
Varnavas
A
A
Department of Pharmaceutical Sciences, University of Trieste, Italy.
Nisi
C
C
Lassiani
L
L
Sava
G
G
Perissin
L
L
Boccù
E
E
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002934:Cinnamates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007700:Kinetics; D008175:Lung Neoplasms / Q000188:drug therapy; D008223:Lymphoma / Q000188:drug therapy; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008815:Mice, Inbred Strains; D010654:Phenylbutyrates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D014226:Triazenes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000970:Antineoplastic Agents; D002934:Cinnamates; D010654:Phenylbutyrates; D014226:Triazenes; C074181:4-(3,3-dimethyl-1-triazeno)phenylbutyric acid; C074180:4-(3,3-dimethyl-1-triazeno)cinnamic acid; C030838:1-(4-carboxyphenyl)-3,3-dimethyltriazene