Peptide chemistry applied to a new family of phenothiazine-containing inhibitors of human farnesyltransferase

GM Dumitriu, A Ghinet, E Bîcu, B Rigo, J Dubois…

文献索引：Dumitriu, Gina-Mirabela; Ghinet, Alina; Bicu, Elena; Rigo, Benoit; Dubois, Joelle; Farce, Amaury; Belei, Dalila Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 14 p. 3180 - 3185

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被引用次数: 11

摘要

Abstract Novel phenothiazine derivatives bearing an amino acid residue were synthesized via peptide chemistry, and evaluated for their inhibitory potential on human farnesyltransferase. The phenothiazine unit proved to be an important bulky unit in the structure of the synthesized inhibitors. Propargyl ester 20 bearing a tyrosine residue exhibited the best biological potential in vitro in the present study. Further syntheses and ...