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Journal of Enzyme Inhibition and Medicinal Chemistry

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https://www.readbyqxmd.com/read/28791908/synthesis-and-biological-evaluation-of-novel-7-hydroxy-4-phenylchromen-2-one-linked-to-triazole-moieties-as-potent-cytotoxic-agents
#1
Chuan-Feng Liu, Qing-Kun Shen, Jia-Jun Li, Yu-Shun Tian, Zheshan Quan
A new series of novel 7-hydroxy-4-phenylchromen-2-one (1a)-linked 1,2,4-triazoles were synthesised using a click chemistry approach. All derivatives were subjected to 3-(4,5-dimethylthiazol-yl)-diphenyl tetrazolium bromide (MTT) cytotoxicity screening against a panel of six different human cancer cell lines (AGS, MGC-803, HCT-116, A-549, HepG2, and HeLa) to assess their cytotoxic potential. Among the tested molecules, some of the analogues showed better cytotoxic activity than that shown by the 7-hydroxy-4-phenylchromen-2-one (1a)...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28791907/a-one-step-procedure-for-immobilising-the-thermostable-carbonic-anhydrase-sspca-on-the-surface-membrane-of-escherichia-coli
#2
Sonia Del Prete, Rosa Perfetto, Mosè Rossi, Fatmah A S Alasmary, Sameh M Osman, Zeid AlOthman, Claudiu T Supuran, Clemente Capasso
The carbonic anhydrase superfamily (CA, EC 4.2.1.1) of metalloenzymes is present in all three domains of life (Eubacteria, Archaea, and Eukarya), being an interesting example of convergent/divergent evolution, with its seven families (α-, β-, γ-, δ-, ζ-, η-, and θ-CAs) described so far. CAs catalyse the simple, but physiologically crucial reaction of carbon dioxide hydration to bicarbonate and protons. Recently, our groups characterised the α-CA from the thermophilic bacterium, Sulfurihydrogenibium yellowstonense finding a very high catalytic activity for the CO2 hydration reaction (kcat = 9...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28783982/quantitative-assessment-of-specific-carbonic-anhydrase-inhibitors-effect-on-hypoxic-cells-using-electrical-impedance-assays
#3
Luciana Stanica, Mihaela Gheorghiu, Miruna Stan, Cristina Polonschii, Sorin David, Dumitru Bratu, Anca Dinischiotu, Claudiu T Supuran, Eugen Gheorghiu
Carbonic anhydrase IX (CA IX) is an important orchestrator of hypoxic tumour environment, associated with tumour progression, high incidence of metastasis and poor response to therapy. Due to its tumour specificity and involvement in associated pathological processes: tumourigenesis, angiogenesis, inhibiting CA IX enzymatic activity has become a valid therapeutic option. Dynamic cell-based biosensing platforms can complement cell-free and end-point analyses and supports the process of design and selection of potent and selective inhibitors...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28776447/analysis-of-imidazoles-and-triazoles-in-biological-samples-after-microextraction-by-packed-sorbent
#4
Cristina Campestre, Marcello Locatelli, Paolo Guglielmi, Elisa De Luca, Giuseppe Bellagamba, Sergio Menta, Gokhan Zengin, Christian Celia, Luisa Di Marzio, Simone Carradori
This paper reports the MEPS-HPLC-DAD method for the simultaneous determination of 12 azole drugs (bifonazole, butoconazole, clotrimazole, econazole, itraconazole, ketoconazole, miconazole, posaconazole, ravuconazole, terconazole, tioconazole and voriconazole) administered to treat different systemic and topical fungal infections, in biological samples. Azole drugs separation was performed in 36 min. The analytical method was validated in the ranges as follows: 0.02-5 μg mL(-1) for ravuconazole; 0.2-5 μg mL(-1) for terconazole; 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28776445/inhibition-of-dengue-virus-replication-by-novel-inhibitors-of-rna-dependent-rna-polymerase-and-protease-activities
#5
Sveva Pelliccia, Yu-Hsuan Wu, Antonio Coluccia, Giuseppe La Regina, Chin-Kai Tseng, Valeria Famiglini, Domiziana Masci, John Hiscott, Jin-Ching Lee, Romano Silvestri
Dengue virus (DENV) is the leading mosquito-transmitted viral infection in the world. With more than 390 million new infections annually, and up to 1 million clinical cases with severe disease manifestations, there continues to be a need to develop new antiviral agents against dengue infection. In addition, there is no approved anti-DENV agents for treating DENV-infected patients. In the present study, we identified new compounds with anti-DENV replication activity by targeting viral replication enzymes - NS5, RNA-dependent RNA polymerase (RdRp) and NS3 protease, using cell-based reporter assay...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28776440/synthesis-biological-activity-and-multiscale-molecular-modeling-studies-for-coumaryl-carboxamide-derivatives-as-selective-carbonic-anhydrase-ix-inhibitors
#6
Belma Zengin Kurt, Fatih Sonmez, Serdar Durdagi, Busecan Aksoydan, Ramin Ekhteiari Salmas, Andrea Angeli, Mustafa Kucukislamoglu, Claudiu T Supuran
New coumaryl-carboxamide derivatives with the thiourea moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and their inhibitory activity against the human carbonic anhydrase (hCA) isoforms hCA I, II, VII and IX were evaluated. While the hCA I, II and VII isoforms were not inhibited by the investigated compounds, the tumour-associated isoform hCA IX was inhibited in the high nanomolar range. 2-Oxo-N-((2-(pyrrolidin-1-yl)ethyl)carbamothioyl)-2H-chromene-3-carboxamide (e11) exhibited a selective inhibitory action against hCA IX with the Ki of 107...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28776438/allosteric-inhibition-of-carnosinase-cn1-by-inducing-a-conformational-shift
#7
Verena Peters, Claus P Schmitt, Tim Weigand, Kristina Klingbeil, Christian Thiel, Antje van den Berg, Vittorio Calabrese, Peter Nawroth, Thomas Fleming, Elisabete Forsberg, Andreas H Wagner, Markus Hecker, Giulio Vistoli
In humans, low serum carnosinase (CN1) activity protects patients with type 2 diabetes from diabetic nephropathy. We now characterized the interaction of thiol-containing compounds with CN1 cysteine residue at position 102, which is important for CN1 activity. Reduced glutathione (GSH), N-acetylcysteine and cysteine (3.2 ± 0.4, 2.0 ± 0.3, 1.6 ± 0.2 µmol/mg/h/mM; p < .05) lowered dose-dependently recombinant CN1 (rCN1) efficiency (5.2 ± 0.2 µmol/mg/h/mM) and normalized increased CN1 activity renal tissue samples of diabetic mice...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28766956/design-and-synthesis-of-benzopyran-based-inhibitors-of-the-hypoxia-inducible-factor-1-pathway-with-improved-water-solubility
#8
Jalisa H Ferguson, Zeus De Los Santos, Saroja N Devi, Stefan Kaluz, Erwin G Van Meir, Sarah K Zingales, Binghe Wang
While progress has been made in treating cancer, cytotoxic chemotherapeutic agents are still the most widely used drugs and are associated with severe side-effects. Drugs that target unique molecular signalling pathways are needed for treating cancer with low or no intrinsic toxicity to normal cells. Our goal is to target hypoxic tumours and specifically the hypoxia inducible factor (HIF) pathway for the development of new cancer therapies. To this end, we have previously developed benzopyran-based HIF-1 inhibitors such as arylsulfonamide KCN1...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28766952/inhibition-of-the-%C3%AE-carbonic-anhydrase-from-the-dandruff-producing-fungus-malassezia-globosa-with-monothiocarbamates
#9
Alessio Nocentini, Daniela Vullo, Sonia Del Prete, Sameh M Osman, Fatmah A S Alasmary, Zeid AlOthman, Clemente Capasso, Fabrizio Carta, Paola Gratteri, Claudiu T Supuran
A series of monothiocarbamates (MTCs) was investigated for the inhibition of the β-class carbonic anhydrase (CAs, EC 4.2.1.1) from the fungal parasite Malassezia globosa, MgCA. These MTCs incorporate various scaffolds, among which aliphatic amine with 1-4 carbons atom in their molecule, morpholine, piperazine, as well as phenethylamine and benzylamine derivatives. All the reported MTCs displayed a better efficacy in inhibiting MgCA compared to the clinically used sulphonamide drug acetazolamide (KI of 74 μM), with KIs spanning between 1...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28762291/water-permeability-is-a-measure-of-severity-in-acute-appendicitis
#10
Nicola Pini, Viktoria A Pfeifle, Urs Kym, Simone Keck, Virginie Galati, Stefan Holland-Cunz, Stephanie J Gros
Acute appendicitis is the most common indication for pediatric abdominal emergency surgery. Determination of the severity of appendicitis on clinical grounds is challenging. Complicated appendicitis presenting with perforation, abscess or diffuse peritonitis is not uncommon. The question remains why and when acute appendicitis progresses to perforation. The aim of this study was to assess the impact of water permeability on the severity of appendicitis. We show that AQP1 expression and water permeability in appendicitis correlate with the stage of inflammation and systemic infection parameters, leading eventually to perforation of the appendix...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28753093/synthesis-and-carbonic-anhydrase-i-ii-vii-and-ix-inhibition-studies-with-a-series-of-benzo-d-thiazole-5-and-6-sulfonamides
#11
Morteza Abdoli, Andrea Angeli, Murat Bozdag, Fabrizio Carta, Ali Kakanejadifard, Hamid Saeidian, Claudiu T Supuran
A series of benzo[d]thiazole-5- and 6-sulfonamides has been synthesized and investigated for the inhibition of several human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms, using ethoxzolamide (EZA) as lead molecule. 2-Amino-substituted, 2-acylamino- and halogenated (bromo-and iodo-derivatives at the heterocyclic ring) compounds led to several interesting inhibitors against the cytosolic hCA I, II and VII, as well as the transmembrane, tumor-associated hCA IX isoforms. Several subnanomolar/low nanomolar, isoform-selective sulfonamide inhibitors targeting hCA II, VII and IX were detected...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28741386/cloning-expression-and-purification-of-the-%C3%AE-carbonic-anhydrase-from-the-mantle-of-the-mediterranean-mussel-mytilus-galloprovincialis
#12
Rosa Perfetto, Sonia Del Prete, Daniela Vullo, Vincenzo Carginale, Giovanni Sansone, Carmela M A Barone, Mosè Rossi, Fatmah A S Alasmary, Sameh M Osman, Zeid AlOthman, Claudiu T Supuran, Clemente Capasso
We cloned, expressed, purified, and determined the kinetic constants of the recombinant α-carbonic anhydrase (rec-MgaCA) identified in the mantle tissue of the bivalve Mediterranean mussel, Mytilus galloprovincialis. In metazoans, the α-CA family is largely represented and plays a pivotal role in the deposition of calcium carbonate biominerals. Our results demonstrated that rec-MgaCA was a monomer with an apparent molecular weight of about 32 kDa. Moreover, the determined kinetic parameters for the CO2 hydration reaction were kcat =  4...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28738705/new-sulfurated-derivatives-of-cinnamic-acids-and-rosmaricine-as-inhibitors-of-stat3-and-nf-%C3%AE%C2%BAb-transcription-factors
#13
Elena Gabriele, Dario Brambilla, Chiara Ricci, Luca Regazzoni, Kyoko Taguchi, Nicola Ferri, Akira Asai, Anna Sparatore
A set of new sulfurated drug hybrids, mainly derived from caffeic and ferulic acids and rosmaricine, has been synthesized and their ability to inhibit both STAT3 and NF-κB transcription factors have been evaluated. Results showed that most of the new hybrid compounds were able to strongly and selectively bind to STAT3, whereas the parent drugs were devoid of this ability at the tested concentrations. Some of them were also able to inhibit the NF-κB transcriptional activity in HCT-116 cell line and inhibited HCT-116 cell proliferation in vitro with IC50 in micromolar range, thus suggesting a potential anticancer activity...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28738704/insights-into-the-binding-mode-of-sulphamates-and-sulphamides-to-hca-ii-crystallographic-studies-and-binding-free-energy-calculations
#14
Giuseppina De Simone, Emma Langella, Davide Esposito, Claudiu T Supuran, Simona Maria Monti, Jean-Yves Winum, Vincenzo Alterio
Sulphamate and sulphamide derivatives have been largely investigated as carbonic anhydrase inhibitors (CAIs) by means of different experimental techniques. However, the structural determinants responsible for their different binding mode to the enzyme active site were not clearly defined so far. In this paper, we report the X-ray crystal structure of hCA II in complex with a sulphamate inhibitor incorporating a nitroimidazole moiety. The comparison with the structure of hCA II in complex with its sulphamide analogue revealed that the two inhibitors adopt a completely different binding mode within the hCA II active site...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28726524/subnanomolar-indazole-5-carboxamide-inhibitors-of-monoamine-oxidase-b-mao-b-continued-indications-of-iron-binding-experimental-evidence-for-optimised-solubility-and-brain-penetration
#15
Nikolay T Tzvetkov, Liudmil Antonov
Pharmacological and physicochemical studies of N-unsubstituted indazole-5-carboxamides (subclass I) and their structurally optimised N1-methylated analogues (subclass II), initially developed as drug and radioligand candidates for the treatment and diagnosis of Parkinson's disease (PD), are presented. The compounds are highly brain permeable, selective, reversible, and competitive monoamine oxidase B (MAO-B) inhibitors with improved water-solubility and subnanomolar potency (pIC50 >8.8). Using a well-validated, combined X-ray/modelling technology platform, we performed a semi-quantitative analysis of the binding modes of all compounds and investigated the role of the indazole N1 position for their MAO-B inhibitory activity...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28726519/cancer-stem-cells-cd133-inhibition-and-cytotoxicity-of-certain-3-phenylthiazolo-3-2-a-benzimidazoles-design-direct-synthesis-crystal-study-and-in-vitro-biological-evaluation
#16
Ghada H Al-Ansary, Wagdy M Eldehna, Hazem A Ghabbour, Sara T A Al-Rashood, Khalid A Al-Rashood, Radwa A Eladwy, Abdullah Al-Dhfyan, Maha M Kabil, Hatem A Abdel-Aziz
Cancer stem cells (CSCs) have been objects of intensive study since their identification in 1994. Adopting a structural rigidification approach, a novel series of 3-phenylthiazolo[3,2-a]benzimidazoles 4a-d was designed and synthesised, in an attempt to develop potent anticancer agent that can target the bulk of tumour cells and CSCs. The anti-proliferative activity of the synthesised compounds was evaluated against two cell lines, namely; colon cancer HT-29 and triple negative breast cancer MDA-MB-468 cell lines...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28719998/beta-lactamase-database-bldb-structure-and-function
#17
Thierry Naas, Saoussen Oueslati, Rémy A Bonnin, Maria Laura Dabos, Agustin Zavala, Laurent Dortet, Pascal Retailleau, Bogdan I Iorga
Beta-Lactamase Database (BLDB) is a comprehensive, manually curated public resource providing up-to-date structural and functional information focused on this superfamily of enzymes with a great impact on antibiotic resistance. All the enzymes reported and characterised in the literature are presented according to the class (A, B, C and D), family and subfamily to which they belong. All three-dimensional structures of β-lactamases present in the Protein Data Bank are also shown. The characterisation of representative mutants and hydrolytic profiles (kinetics) completes the picture and altogether these four elements constitute the essential foundation for a better understanding of the structure-function relationship within this enzymes family...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28718686/kinetic-study-on-the-inhibition-of-xanthine-oxidase-by-acylated-derivatives-of-flavonoids-synthesised-enzymatically
#18
Maria Elisa Melo Branco de Araújo, Yollanda Edwirges Moreira Franco, Thiago Grando Alberto, Marcia Cristina Fernandes Messias, Camila Wielewski Leme, Alexandra Christine Helena Frankland Sawaya, Patricia de Oliveira Carvalho
Studies have reported that flavonoids inhibit xanthine oxidase (XO) activity; however, poor solubility and stability in lipophilic media limit their bioavailability and applications. This study evaluated the kinetic parameters of XO inhibition and partition coefficients of flavonoid esters biosynthesised from hesperidin, naringin, and rutin via enzymatic acylation with hexanoic, octanoic, decanoic, lauric, and oleic acids catalysed by Candida antarctica lipase B (CALB). Quantitative determination by ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) showed higher conversion yields (%) for naringin and rutin esters using acyl donors with 8C and 10C...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28718678/discovery-of-novel-isoflavone-derivatives-as-ache-buche-dual-targeted-inhibitors-synthesis-biological-evaluation-and-molecular-modelling
#19
Bo Feng, Xinpeng Li, Jie Xia, Song Wu
AChE and BuChE are druggable targets for the discovery of anti-Alzheimer's disease drugs, while dual-inhibition of these two targets seems to be more effective. In this study, we synthesised a series of novel isoflavone derivatives based on our hit compound G from in silico high-throughput screening and then tested their activities by in vitro AChE and BuChE bioassays. Most of the isoflavone derivatives displayed moderate inhibition against both AChE and BuChE. Among them, compound 16 was identified as a potent AChE/BuChE dual-targeted inhibitor (IC50: 4...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28718674/design-and-synthesis-of-a-novel-photoaffinity-probe-for-labelling-egf-receptor-tyrosine-kinases
#20
You-Guang Zheng, Xiao-Qing Wu, Jun Su, Ping Jiang, Liang Xu, Jian Gao, Bin Cai, Min Ji
The epidermal growth factor receptor (EGFR) and HER2 are two important tyrosine kinases that play crucial roles in signal transduction pathways that regulate numerous cellular functions including proliferation, differentiation, migration, and angiogenesis. In the past 20 years, many proteomic methods have emerged as powerful methods to evaluate proteins in biological processes and human disease states. Among them, activity-based protein profiling (ABPP) is one useful approach for the functional analysis of proteins...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
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