Patent Evaluation: Citraconic derivatives as farnesyl protein transferase inhibitors

Abstract

Novelty: Novel farnesyl-protein transferase (FTase) inhibitors are claimed as antitumour agents. By adjusting the compound dosage, FTase activity and the farnesylation of the protein Ras may be reduced only, which has the advantage of avoiding side-effects. The compounds are potentially useful for the treatment of colorectal carcinoma, exocrine pancreatic carcinoma and rnyeloid leukaemias.

Biology: A protocol for measuring in vitro inhibition of Ras FI'ase is detailed but no results are provided.

Chemistry: Synthesis of compounds and their salts was by conventional methods exemplified in eight cases and one scheme. Only the two specified compounds are specifically claimed.