1322757-83-4Relevant academic research and scientific papers
SNAr and palladium-catalyzed reactions of deactivated thiophene: Application to the synthesis of protein farnesyltransferase inhibitors
Lethu, Sebastien,Dubois, Joelle
, p. 3920 - 3931 (2011/09/14)
To investigate the influence of the 5-thioether moiety of our previously identified hit thiophene compound upon protein farnesyltransferase inhibition, we synthesized a new library of 3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic derivatives through the application of aromatic nucleophilic substitutions benefiting from a sulfone-based leaving group and by direct palladium-catalyzed reactions on a thioalkylthiophene. This small library of ester derivatives and their corresponding acids was then evaluated for protein farnesyltransferase inhibitory activity; some library members exhibited promising submicromolar activities. Copyright
