New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis

Lethu, Sébastien; Bosc, Damien; Mouray, Elisabeth; Grellier, Philippe; Dubois, Joëlle

doi:10.3109/14756366.2011.643302

Cited by 28 publications

(18 citation statements)

References 36 publications

(40 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A new synthetic pathway was devised to reach tetrasubstituted 3-arylthiophene 2-carboxylic acids in a three-step solid-phase synthesis. This very efficient methodology provided more than 20 new compounds that were evaluated for their ability to inhibit protein farnesyltransferase from different species as well as Trypanosoma brucei and P. falciparum proliferation [34]. …”

Section: Antimalarial Compounds Against Isoprenoid Biosynthetic Pamentioning

confidence: 99%

Exploring Drug Targets in Isoprenoid Biosynthetic Pathway forPlasmodium falciparum

Qidwai¹,

Jamal

Khan

et al. 2014

Biochemistry Research International

View full text Add to dashboard Cite

Emergence of rapid drug resistance to existing antimalarial drugs in Plasmodium falciparum has created the need for prediction of novel targets as well as leads derived from original molecules with improved activity against a validated drug target. The malaria parasite has a plant plastid-like apicoplast. To overcome the problem of falciparum malaria, the metabolic pathways in parasite apicoplast have been used as antimalarial drug targets. Among several pathways in apicoplast, isoprenoid biosynthesis is one of the important pathways for parasite as its multiplication in human erythrocytes requires isoprenoids. Therefore targeting this pathway and exploring leads with improved activity is a highly attractive approach. This report has explored progress towards the study of proteins and inhibitors of isoprenoid biosynthesis pathway. For more comprehensive analysis, antimalarial drug-protein interaction has been covered.

show abstract

Section: Antimalarial Compounds Against Isoprenoid Biosynthetic Pamentioning

confidence: 99%

Exploring Drug Targets in Isoprenoid Biosynthetic Pathway forPlasmodium falciparum

Qidwai¹,

Jamal

Khan

et al. 2014

Biochemistry Research International

View full text Add to dashboard Cite

show abstract

“…In all experiments, log-phase parasite cultures were harvested by centrifugation at 3000Âg and immediately used. Drug assays were based on the conversion of a redox-sensitive dye (resazurin) to a fluorescent product by viable cells as previously described [45]. Drug stock solutions were prepared in pure DMSO.…”

Section: Anti-trypanosomal Activity Assaymentioning

confidence: 99%

Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones

Havrylyuk

Zimenkovsky

Vasylenko

et al. 2013

European Journal of Medicinal Chemistry

Self Cite

View full text Add to dashboard Cite

A series of novel 5-pyrazoline substituted 4-thiazolidinones have been synthesized. Target compounds were evaluated for their anticancer activity in vitro within DTP NCI protocol. Among the tested compounds, the derivatives 4d and 4f were found to be the most active, which demonstrated certain sensitivity profile toward the leukemia subpanel cell lines with GI₅₀ value ranges of 2.12-4.58 μM (4d) and 1.64-3.20 μM (4f). The screening of antitrypanosomal and antiviral activities of 5-(3-naphthalen-2-yl-5-aryl-4,5-dihydropyrazol-1-yl)-thiazolidine-2,4-diones was carried out with the promising influence of the mentioned compounds on Trypanosoma brucei, but minimal effect on SARS coronavirus and influenza types A and B viruses.

show abstract

“…Drug assays were based on the conversion of a redox-sensitive dye (resazurin) to a fluorescent product by viable cells as described previously. 16 Compounds were first tested at concentrations of 10 and 1 lg/mL (Table 1) and IC 50 s were determined 17 for the most active ones ( Table 2).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antitrypanosomal activity of new 6,6,7-trisubstituted thiopyrano[2,3-d][1,3]thiazoles

Zelisko

Atamanyuk

Vasylenko³

et al. 2012

Bioorganic & Medicinal Chemistry Letters

Self Cite

View full text Add to dashboard Cite

New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis

Cited by 28 publications

References 36 publications

Exploring Drug Targets in Isoprenoid Biosynthetic Pathway forPlasmodium falciparum

Exploring Drug Targets in Isoprenoid Biosynthetic Pathway forPlasmodium falciparum

Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones

Synthesis and antitrypanosomal activity of new 6,6,7-trisubstituted thiopyrano[2,3-d][1,3]thiazoles

Contact Info

Product

Resources

About