New farnesyltransferase inhibitors in the phenothiazine series

D Belei, C Dumea, A Samson, A Farce, J Dubois…

Index: Belei, Dalila; Dumea, Carmen; Samson, Alexandrina; Farce, Amaury; Dubois, Joelle; Bicu, Elena; Ghinet, Alina Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4517 - 4522

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Citation Number: 28

Abstract

The biological screening of the chemical library of our Organic Chemistry Department, carried out on an automated fluorescence-based FTase assay, allowed us to discover that a phenothiazine derivative (1d) was an inhibitor of farnesyltransferase. Three new series of human farnesyltransferase inhibitors, based on a phenothiazine scaffold, were synthesized with protein farnesyltransferase inhibition potencies in the low micromolar range. Ester ...