Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral compounds. Issue 20 (15th October 2015)

• Record Type: Journal Article
• Authors: Dumitriu, Gina-Mirabela; Bîcu, Elena; Belei, Dalila; Rigo, Benoît; Dubois, Joëlle; Farce, Amaury; Ghinet, Alina
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 20(2015)
• Page Start: 4447
• Page End: 4452
• Publication Date: 2015-10-15
• Subjects: Farnesyltransferase -- Phenothiazine -- Cysteine -- Methionine -- Serine -- Valine -- CAAX inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.09.008
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A new family of CaaX competitive inhibitors of human farnesyltransferase based on phenothiazine and carbazole skeleton bearing al -cysteine, l -methionine, l -serine orl -valine moiety was designed, synthesized and biologically evaluated. Phenothiazine derivatives proved to be more active than carbazole-based compounds. Phenothiazine1b with cysteine residue was the most promising inhibitor of human farnesyltransferase in the current study.