Search Results - "Bouaziz, Zouhair"
-
1
Carbazole scaffolds in cancer therapy: a review from 2012 to 2018
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2019)“…For over half a century, the carbazole skeleton has been the key structural motif of many biologically active compounds including natural and synthetic…”
Get full text
Journal Article -
2
Mechanistic basis of breast cancer resistance protein inhibition by new indeno[1,2-b]indoles
Published in Scientific reports (19-01-2021)“…The ATP-binding cassette transporter ABCG2 mediates the efflux of several chemotherapeutic drugs, contributing to the development of multidrug resistance (MDR)…”
Get full text
Journal Article -
3
Solubility enhancement of mefenamic acid by inclusion complex with β-cyclodextrin: in silico modelling, formulation, characterisation, and in vitro studies
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2021)“…The aim of this study was to prepare and characterise inclusion complexes of a low water-soluble drug, mefenamic acid (MA), with β-cyclodextrin (β-CD). First,…”
Get full text
Journal Article -
4
Microwave-accelerated multicomponent synthesis and X-ray characterization of novel benzothiadiazinone dioxide derivatives, analogues of Monastrol
Published in Research on chemical intermediates (01-04-2021)“…We demonstrate here a rapid and comfortable synthetic sequence to benzothiadiazinone dioxide (six-membered cyclic sulfamide) derivatives, analogues of…”
Get full text
Journal Article -
5
QSAR Model of Indeno[1,2- b ]indole Derivatives and Identification of N -isopentyl-2-methyl-4,9-dioxo-4,9-Dihydronaphtho[2,3- b ]furan-3-carboxamide as a Potent CK2 Inhibitor
Published in Molecules (Basel, Switzerland) (01-01-2020)“…Casein kinase II (CK2) is an intensively studied enzyme, involved in different diseases, cancer in particular. Different scaffolds were used to develop…”
Get full text
Journal Article -
6
Broad-Spectrum Anticancer Activity and Pharmacokinetic Properties of a Prenyloxy-Substituted Indeno[1,2-b]indole Derivative, Discovered as CK2 Inhibitor
Published in Pharmaceuticals (Basel, Switzerland) (05-06-2021)“…Protein kinase CK2 is involved in regulating cellular processes, such as cell cycle, proliferation, migration, and apoptosis, making it an attractive…”
Get full text
Journal Article -
7
Synthesis, Spectroscopic Characterization, and In Vitro Antibacterial Evaluation of Novel Functionalized Sulfamidocarbonyloxyphosphonates
Published in Molecules (Basel, Switzerland) (10-07-2018)“…Several new sulfamidocarbonyloxyphosphonates were prepared in two steps, namely carbamoylation and sulfamoylation, by using chlorosulfonyl isocyanate (CSI),…”
Get full text
Journal Article -
8
Development of Pharmacophore Model for Indeno[1,2-b]indoles as Human Protein Kinase CK2 Inhibitors and Database Mining
Published in Pharmaceuticals (Basel, Switzerland) (09-01-2017)“…Protein kinase CK2, initially designated as casein kinase 2, is an ubiquitously expressed serine/threonine kinase. This enzyme, implicated in many cellular…”
Get full text
Journal Article -
9
Inhibition of Shiga toxin-converting bacteriophage development by novel antioxidant compounds
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2018)“…Oxidative stress may be the major cause of induction of Shiga toxin-converting (Stx) prophages from chromosomes of Shiga toxin-producing Escherichia coli…”
Get full text
Journal Article -
10
Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structures with the Catalytic Subunit CK2α and Its Paralog CK2α
Published in Pharmaceuticals (Basel, Switzerland) (13-12-2017)“…Protein kinase CK2, a member of the eukaryotic protein kinase superfamily, is associated with cancer and other human pathologies and thus an attractive drug…”
Get full text
Journal Article -
11
Synthesis, X-ray structure, in silico calculation, and carbonic anhydrase inhibitory properties of benzylimidazole metal complexes
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2018)“…Three coordination compounds of formula {M(bmim) 2 Cl 2 } were synthetised (M = Co, Zn, and Hg) and fully characterised. Each complex incorporates…”
Get full text
Journal Article -
12
Diacritic Binding of an Indenoindole Inhibitor by CK2α Paralogs Explored by a Reliable Path to Atomic Resolution CK2α′ Structures
Published in ACS omega (31-03-2019)“…CK2α and CK2α′ are the two isoforms of the catalytic subunit of human protein kinase CK2, an important target for cancer therapy. They have similar, albeit not…”
Get full text
Journal Article -
13
Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2
Published in Pharmaceuticals (Basel, Switzerland) (08-06-2015)“…Due to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design of ATP-competitive inhibitors of human CK2…”
Get full text
Journal Article -
14
Self-Assembled Supramolecular Nanoparticles Improve the Cytotoxic Efficacy of CK2 Inhibitor THN7
Published in Pharmaceuticals (Basel, Switzerland) (26-01-2018)“…Since the approval of imatinib in 2001, kinase inhibitors have revolutionized cancer therapies. Inside this family of phosphotransferases, casein kinase 2…”
Get full text
Journal Article -
15
Crystal structure of 13-(2-methoxyphenyl)-3,4-dihydro-2H-indazolo[1,2-b]phthalazine-1,6,11(13H)-trione
Published in Acta crystallographica. Section E, Crystallographic communications (01-08-2015)“…In the title compound, C22H18N2O4, the three fused rings of the pyrazolophthalazine moiety are coplanar (r.m.s. deviation = 0.027 Å). The cyclohexene ring…”
Get full text
Journal Article -
16
Methyl 3-(Quinolin-2-yl)indolizine-1-carboxylate
Published in MolBank (01-03-2016)“…A novel compound, methyl 3-(quinolin-2-yl)indolizine-1-carboxylate (2) has been synthesized by cycloaddition reaction of 1-(quinolin-2-ylmethyl)pyridinium…”
Get full text
Journal Article -
17
Crystal structure of 13-phenyl-2,3,4,13-tetrahydro-1H-indazolo[1,2-b]phthalazine-1,6,11-trione
Published in Acta crystallographica. Section E, Crystallographic communications (01-12-2015)“…The title compound, C21H16N2O3, consists of an indazolone moiety, bearing a phenyl group, fused to a phthalazine ring system (r.m.s. deviation = 0.018 Å). The…”
Get full text
Journal Article -
18
Synthesis and Diels–Alder Reactivity of ortho-Carbazolequinones
Published in Chemical & Pharmaceutical Bulletin (01-09-2004)“…Oxidation of 2- and 3-hydroxycarbazoles with Frémy's salt gave the corresponding ortho-carbazolequinones. These molecules react as carbodienophiles in…”
Get full text
Journal Article -
19
Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion
Published in European journal of medicinal chemistry (01-01-2021)“…Ninhydrins show extensive application in organic chemistry and agriculture whereas they have been poorly investigated as bioactive molecules for medicinal…”
Get full text
Journal Article -
20
Carbazolequinone induction of caspase-dependent cell death in Src-overexpressing cells
Published in Biochemical pharmacology (01-12-2002)“…We previously reported that RSV-transformed quail neuroretina cells (QNR-ts68) were highly resistant to apoptosis provoked by serum withdrawal, and that this…”
Get full text
Journal Article