Patent Evaluation: Heterocyclic sulphonylureas as antitumour agents

Summary

Novelty: Heterocyclic sulphonylureas are claimed to possess broad-spectrum antitumour activity.

Biology: Antitumour activity is demonstrated against transplantable solid murine tumours in vivo, in particular lymphosarcoma 6C3HED borne by C3H mice. The compounds, administered at a dose of 300 mg/kg po, show almost total inhibition of tumour growth and an improvement in mortality in comparison with control.

Chemistry: Syntheses of the compounds are by conventional methods, outlined in a multi-step preparative scheme and forming a subsidiary part of the claim. Twenty-three compounds are exemplified, and several are specifically claimed including N-[[(4-chlorophenyl)amino]-carbonyl]-4,5-dimethyl-2-thiophenesulphonamide.

Structure: