Synthesis and biological evaluation of a new series of phenothiazine-containing protein farnesyltransferase inhibitors.

Autor: Abuhaie CM; Department of Organic Chemistry, Al. I. Cuza University of Iasi, Faculty of Chemistry, Bd. Carol I nr. 11, 700506 Iasi, Romania., Ghinet A, Farce A, Dubois J, Gautret P, Rigo B, Belei D, Bîcu E
Jazyk: angličtina
Zdroj: European journal of medicinal chemistry [Eur J Med Chem] 2013 Jan; Vol. 59, pp. 101-10. Date of Electronic Publication: 2012 Nov 14.
DOI: 10.1016/j.ejmech.2012.11.008
Abstrakt: Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC(50) values of 0.7 and 0.6 μM, respectively.
(Copyright © 2012 Elsevier Masson SAS. All rights reserved.)
Databáze: MEDLINE