Quantitative structure-activity relationships of antitumor guanidinothiazolecarboxamides with survival enhancement for therapy in the 3LL Lewis lung carcinoma model

Guanidinothiazolecarboxamides (GTCs) are a novel class of antitumor agents found to be systemically active against experimental pulmonary metastases of 3LL Lewis lung carcinoma. A series of substituted benzothiazole GTCs were found to produce enhancement of survival in this model by using 8 days of...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1991-07, Vol.34 (7), p.1975-1982
Main Authors: Schnur, Rodney C, Gallaschun, Randall J, Singleton, David H, Grissom, Martin, Sloan, Donald E, Goodwin, Peter, McNiff, Patricia A, Fliri, Anton F. J, Mangano, F. Michael
Format: Article
Language:English
Subjects:
Adenocarcinoma - drug therapy
Adenocarcinoma - mortality
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - therapeutic use
Biological and medical sciences
Chemical Phenomena
Chemistry
Female
General aspects
Guanidines - chemical synthesis
Guanidines - therapeutic use
Lung Neoplasms - drug therapy
Lung Neoplasms - mortality
Medical sciences
Mice
Models, Biological
Neoplasms, Experimental - drug therapy
Neoplasms, Experimental - mortality
Pharmacology. Drug treatments
Structure-Activity Relationship
Thiazoles - chemical synthesis
Thiazoles - therapeutic use
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Summary:Guanidinothiazolecarboxamides (GTCs) are a novel class of antitumor agents found to be systemically active against experimental pulmonary metastases of 3LL Lewis lung carcinoma. A series of substituted benzothiazole GTCs were found to produce enhancement of survival in this model by using 8 days of intraperitoneal dosing initiated 2 days after intravenous tumor challenge. Quantitative structure-activity relationships have been discovered in the GTC series with survival enhancement correlated to substituent parameters. Optimal correlations were found between the probit transform of the drug-induced increased lifespan (ILS) and field and pi parameters. Among the most effective analogues in this series was N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxam ide.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00111a009