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
… We then investigated the possibility of obtaining phenothiazine-containing FTIs able to
coordinate with the zinc atom of the protein via chelating groups and to interact with the A 2 …

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
… We then investigated the possibility of obtaining phenothiazine-containing FTIs able to
coordinate with the zinc atom of the protein via chelating groups and to interact with the A 2 …

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
… This highlights the importance of the phenothiazine moiety and explains the higher affinity
towards human FTase obtained with phenothiazine-containing ylides 17 compared to …

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
… In this study, we have synthesized and evaluated new … -Tyr) unit as human farnesyltransferase
inhibitors. These structural … in vitro inhibition activities in the micromolar range. Propargyl …

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
… described for the first time phenothiazinecontaining inhibitors of protein farnesyltransferase
(FTase) [… thiol group for a set of proteins, causing their localization on the plasma membrane. …

Farnesyltransferase inhibitors: a comprehensive review based on quantitative structural analysis

N SHN Moorthy, SF Sousa, MJ Ramos… - Current medicinal …, 2013 - ingentaconnect.com
… 1 from compound 1 to 24) and benzonitrile analogs (series 2 from compound 25 to 66) by
Deeb et al., [177]. This research group proposed four compounds from the analysis, which had …

The recent development of farnesyltransferase inhibitors as anticancer and antimalarial agents

Y Shen, S Qiang, S Ma - Mini Reviews in Medicinal Chemistry, 2015 - ingentaconnect.com
… Search for protein farnesyltransferase inhibitors of microbial origin: our strategy and results
as well as the results obtained by … Farnesyltransferase inhibitors inhibit the growth of malaria …

[HTML][HTML] Pegylation of phenothiazine–A synthetic route towards potent anticancer drugs

S Cibotaru, V Nastasa, AI Sandu, AC Bostanaru… - Journal of Advanced …, 2022 - Elsevier
… Starting from these premises, our group designed PEGylated phenothiazine derivatives
as new building blocks for anticancer drugs. PEG has been bonded to the phenothiazine …

Antitumor Activity of PEGylated and TEGylated Phenothiazine Derivatives: Structure–Activity Relationship

S Cibotaru, AI Sandu, A Nicolescu, L Marin - International Journal of …, 2023 - mdpi.com
… into researcher attention another potential anticancer mechanism, that is, inhibition of
enzymes with a key role in tumor cell proliferation, such as farnesyltransferase [26,29,30,31]. …

FTase inhibitors and cancer: prospects for use in targeted therapies

M Xia, L Yu, Z Yan, Y Wang, L Zhang, G Miao… - Medicinal Chemistry …, 2024 - Springer
… The bivalent compound 8 containing guanidine was synthesized with FTI-276, and biological
evaluation showed that the methyl ester form compound 8b could inhibit the formation of …