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

CM Abuhaie, A Ghinet, A Farce, J Dubois… - European Journal of …, 2013 - Elsevier
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 …

Investigation of New Phenothiazine and Carbazole Derivatives as Potential Inhibitors of Human Farnesyltransferase

GM Dumitriu, A Ghinet, D Belei, B Rigo… - Letters in Drug …, 2015 - ingentaconnect.com
A new series of phenothiazine and carbazole derivatives was synthesized and evaluated for
their biological activity on human protein farnesyltransferase. The farnesyltransferase …

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

GM Dumitriu, A Ghinet, E Bîcu, B Rigo, J Dubois… - Bioorganic & Medicinal …, 2014 - Elsevier
Novel phenothiazine derivatives bearing an amino acid residue were synthesized via
peptide chemistry, and evaluated for their inhibitory potential on human farnesyltransferase …

New farnesyltransferase inhibitors in the phenothiazine series

D Belei, C Dumea, A Samson, A Farce, J Dubois… - Bioorganic & medicinal …, 2012 - Elsevier
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 …

Synthesis and biological evaluation of new phenothiazine derivatives bearing a pyrazole unit as protein farnesyltransferase inhibitors

L Baciu-Atudosie, A Ghinet, A Farce, J Dubois… - Bioorganic & medicinal …, 2012 - Elsevier
A new family of protein farnesyltransferase inhibitors, based on a phenothiazine scaffold,
was designed and synthesized. The biological evaluation of these products showed that …

New indolizine–chalcones as potent inhibitors of human farnesyltransferase: design, synthesis and biological evaluation

IM Moise, A Ghinet, D Belei, J Dubois, A Farce… - Bioorganic & Medicinal …, 2016 - Elsevier
A new family of indolizine–chalcones was designed, synthesized and screened for the
inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents …

Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral …

GM Dumitriu, E Bîcu, D Belei, B Rigo, J Dubois… - Bioorganic & Medicinal …, 2015 - Elsevier
A new family of CaaX competitive inhibitors of human farnesyltransferase based on
phenothiazine and carbazole skeleton bearing a l-cysteine, l-methionine, l-serine or l-valine …

Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors

CM Abuhaie, A Ghinet, A Farce, J Dubois… - Bioorganic & medicinal …, 2013 - Elsevier
A new family of 30 benzoylated N-ylides 4 and 5 was synthesized and evaluated for the
inhibitory activity on human protein farnesyltransferase. Most of these novel compounds …

Discovery of a new class of protein farnesyltransferase inhibitors in the arylthiophene series

S Lethu, M Ginisty, D Bosc, J Dubois - Journal of medicinal …, 2009 - ACS Publications
Screening of the ICSN chemical library led to the discovery of 3-(4-chlorophenyl)-4-cyano-5-
thioalkylthiophene 2-carboxylic acids as potent farnesyltransferase inhibitors. Enzymatic …

Impact on farnesyltransferase inhibition of 4-chlorophenyl moiety replacement in the Zarnestra® series

P Angibaud, L Mevellec, C Meyer, X Bourdrez… - European journal of …, 2007 - Elsevier
Based on the structure of R115777 (tipifarnib, Zarnestra®), a series of farnesyltransferase
inhibitors have been synthesized by modification of the 2-quinolinone motif and …