Quantitative Structure-Activity Relationsships of Antitumor Guanidinothiazolecarboxamides with Survival Enhancement for Therapy in the 3LL Lewis Lung Carcinoma Model

Article abstract of DOI:10.1021/jm00111a009

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 ? parameters.Among the most effective analogues in this series was N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxamide (19).