Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.

abstract：:A series of N1-(substituted)aryl-5,7-dimethyl-2-(substituted)pyrido(2,3-d)pyrimidin-4(3H)-one was designed on the basis of the triangular pharmacophoric requirement of histamine H1-receptor antagonists. The designed series was synthesized by cyclo-condensation of monoaryl thiourea with ethyl cyanoacetate in the presen...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Suhagia BN,Chhabria MT,Makwana AG

更新日期：2006-12-01 00:00:00

abstract：:The reaction mechanism of glycoside hydrolases belonging to family 1 (GH1) of carbohydrate-active enzymes classification, hydrolysing β-O-glycosidic bonds, is well characterised. This family includes several thousands of enzymes with more than 20 different EC numbers depending on the sugar glycone recognised as substr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Strazzulli A,Perugino G,Mazzone M,Rossi M,Withers SG,Moracci M

更新日期：2019-12-01 00:00:00

abstract：:The flip regression procedure that we used earlier for handling the xanthones system has been applied to phenylaminoquinazoline analogues. It is known that the substituents at the 6- and 7- positions of the polycyclic system have been identified as the most important structural features. The steric as well as the elec...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Deeb O,Clare BW

更新日期：2008-12-01 00:00:00

abstract：:In this study, firstly, antioxidant and polyphenol oxidase (PPO) properties of Yomra apple were investigated. Seventeen phenolic constituents were measured by reverse phase-high-performance liquid chromatography (RP-HPLC). Total phenolic compounds (TPCs), ferric reducing antioxidant power (FRAP) and 2, 2-diphenyl-1-pi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Can Z,Dincer B,Sahin H,Baltas N,Yildiz O,Kolayli S

更新日期：2014-12-01 00:00:00

abstract：:Indoleamine 2,3-dioxygenase 1 (IDO1) activity links to immune escape of cancers. Inhibition of IDO1 provides a new approach for cancer treatment. Most clinical IDO1 drugs show marginal efficacy as single agents. On basis of molecular docking and pharmacophore modelling, a novel inhibitor Roxyl-WL was discovered with a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Xu G,Wang T,Li Y,Huang Z,Wang X,Zheng J,Yang S,Fan Y,Xiang R

更新日期：2018-12-01 00:00:00

abstract：:Analogs of pralidoxime, which is a commercial antidote for intoxication from neurotoxic organophosphorus compounds, were designed, synthesized, characterized, and tested as potential inhibitors or reactivators of acetylcholinesterase (AChE) using the Ellman's test, nuclear magnetic resonance, and molecular modeling. T...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Petronilho Eda C,Rennó Mdo N,Castro NG,da Silva FM,Pinto Ada C,Figueroa-Villar JD

更新日期：2016-12-01 00:00:00

abstract：:Exposure of the N-methoxycarbonyl-bicyclic-keto-acid 5 (improved preparation) to the Barnick beta-keto-acid synthesis yielded an aqueous solution of the sodium salts of the beta-keto-acids 26 and 27 which on heating at 60-65 degrees C furnished the N-methoxycarbonyl-tricyclic-ketone 9 (55%) plus the hydroxy-ketone 28 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bowman MA,Bowman RE,Davies RV,Haran G,Harris PJ,Smith HJ,Steele RW,Walker N,Whiting K

更新日期：2002-06-01 00:00:00

abstract：:The current study was designed to assess the inhibitory activity of Broussonetia papyrifera-derived polyphenols against 3-chymotrypsin-like and papain-like coronavirus cysteine proteases. The isolated compounds were broussochalcone B (1), broussochalcone A (2), 4-hydroxyisolonchocarpin (3), papyriflavonol A (4), 3'-(3...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Park JY,Yuk HJ,Ryu HW,Lim SH,Kim KS,Park KH,Ryu YB,Lee WS

更新日期：2017-12-01 00:00:00

abstract：:Recently we found that 1-methyldodecanoylindole-2-carboxylic acid (1) and 1-[2-(4-carboxyphenoxy)ethyl]-3-dodecanoylindole-2-carboxylic acid (4) were inhibitors of the cytosolic phospholipase A2alpha (cPLA2alpha)-mediated arachidonic acid release in calcium ionophore A23187-stimulated human platelets with IC50-values ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ghasemi A,Elfringhoff AS,Lehr M

更新日期：2005-10-01 00:00:00

abstract：:Monoacylglycerol lipase is a serine hydrolase that plays a major role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol. A wide number of MAGL inhibitors are reported in literature; however, many of them are characterised by an irreversible mechanism of action and this behavior determin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Granchi C,Caligiuri I,Bertelli E,Poli G,Rizzolio F,Macchia M,Martinelli A,Minutolo F,Tuccinardi T

更新日期：2017-12-01 00:00:00

abstract：:The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and new antimycobacterial compound development. For this purpose, new triazoles were synthesized and evaluated for antituberculosis activity. A series of 4-arylidenamino-4H-1,2,4-triazol...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozdemir A,Turan-Zitouni G,Kaplancikli ZA,Chevallet P

更新日期：2007-08-01 00:00:00

abstract：:A new series of tertiary amine derivatives of chlorochalcone (4a∼4l) were designed, synthesized and evaluated for the effect on acetylcholinesterase (AChE) and buthylcholinesterase (BuChE). The results indicated that all compounds revealed moderate or potent inhibitory activity against AChE, and some possessed high se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gao XH,Zhou C,Liu HR,Liu LB,Tang JJ,Xia XH

更新日期：2017-12-01 00:00:00

abstract：:Structure modification of the side chain of the lead compound benzoxanthone provided a series of benzoxanthone analogues and 12 of them were first reported. The results showed that most of these compounds had moderate cytotoxicity against tumour cells with the 50% inhibition concentration in the micromolar range. Furt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cheng P,Zhu L,Guo W,Liu W,Yao J,Dong G,Zhang Y,Zhuang C,Sheng C,Miao Z,Zhang W

更新日期：2012-06-01 00:00:00

abstract：:Numerous studies have highlighted the implications of the glycogen synthase kinase 3 (GSK-3) in several processes associated with Alzheimer's disease (AD). Therefore, GSK-3 has become a crucial therapeutic target for the treatment of this neurodegenerative disorder. Hereby, we report the design and multistep synthesis...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sciú ML,Sebastián-Pérez V,Martinez-Gonzalez L,Benitez R,Perez DI,Pérez C,Campillo NE,Martinez A,Moyano EL

更新日期：2019-12-01 00:00:00

abstract：:Initial velocity enzyme kinetics was used to study the inhibition mechanism of guanidine hydrochloride (Gdm.Cl) on catalytic activity of recombinant human protein disulfide isomerase (rhPDI) in protein folding. Reduced C125A recombinant human interleukin 2 (C125A rhIL-2), the substrate, was dissolved in 8 M Gdm.Cl bef...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Du C,Wolfe JL

更新日期：2003-02-01 00:00:00

abstract：:Quantitative structure-activity relationships (QSARs) within a series of cytochrome P450 2C9 (CYP2C9) and cytochrome P450 2C19 (CYP2C19) inhibitors are reported. In particular, it is noted that compound lipophilicity, in the form of log P values (where P is the octanol/water partition coefficient), is an important fac...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lewis DF,Lake BG,Ito Y,Dickins M

更新日期：2006-08-01 00:00:00

abstract：:Several 2,5-disubstituted-1,3,4-oxadiazoles (4a-f) and 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles (7a-f) were synthesized and characterized by elemental analyses and spectral data. These compounds were screened for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. Compo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chawla G,Kumar U,Bawa S,Kumar J

更新日期：2012-10-01 00:00:00

abstract：:Reaction of thiophosgene with 4-aminomethyl-benzenesulfonamide afforded 4-isothiocyanatomethyl-benzenesulfonamide, which by reaction with amines, amino acids and oligopeptides, lead to a series of new sulfonamides incorporating a 4-sulfamoylphenylmethylthiourea scaffold. These new thioureas showed strong affinities to...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Casini A,Scozzafava A,Mincione F,Menabuoni L,Supuran CT

更新日期：2002-10-01 00:00:00

abstract：:The two β-carbonic anhydrases (CAs, EC 4.2.1.1) recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 aromatic, heterocyclic, and aliphatic sulfonamides and one sulfamate, many of which are clinically used agents. CAS1 was ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vullo D,Lehneck R,Pöggeler S,Supuran CT

更新日期：2018-12-01 00:00:00

abstract：UNLABELLED:Context: Garcinia hombroniana Pierre, known as manggis hutan in Malaysia is a rich source of xanthones and benzophenones. OBJECTIVES:This study was aimed to isolate and characterize potential cholinesterase inhibitors from the extracts of G. hombroniana bark and investigate their interactions with the enzym...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jamila N,Khairuddean M,Yeong KK,Osman H,Murugaiyah V

更新日期：2015-02-01 00:00:00

abstract：:We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 ± 0.05 nM), mode...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pachón-Angona I,Refouvelet B,Andrýs R,Martin H,Luzet V,Iriepa I,Moraleda I,Diez-Iriepa D,Oset-Gasque MJ,Marco-Contelles J,Musilek K,Ismaili L

更新日期：2019-12-01 00:00:00

abstract：:The aims of this study were to examine the antiproliferation of Humulus lupulus extracts on human hepatoma carcinoma (Hep3B) and human colon carcinoma (HT-29) cell lines along with enzyme inhibitory effects of the crude extracts. Potential cell cytotoxicity of six different H. lupulus extracts were assayed on various ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cömert Önder F,Ay M,Aydoğan Türkoğlu S,Tura Köçkar F,Çelik A

更新日期：2016-01-01 00:00:00

abstract：:The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was c...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gökçe B,Gençer N,Arslan O,Turkoğlu SA,Alper M,Köçkar F

更新日期：2012-02-01 00:00:00

abstract：:Corticosteroids are anti-inflammatory drugs that are similar to the natural corticosteroid hormones produced by the cortex of the adrenal glands. The objective of this study was to scrutinize effects of some corticosteroids on glucose-6-phosphate dehydrogenase (G6PD) and some antioxidant enzymes. Initially, G6PD was p...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozmen I

更新日期：2005-02-01 00:00:00

abstract：:A series of hydroxylic compounds (1-10, NK-154 and NK-168) have been assayed for the inhibition of three physiologically relevant carbonic anhydrase isozymes, the cytosolic isozymes I, II and tumor-associated isozyme IX. The investigated compounds showed inhibition constants in the range of 0.068-4003, 0.012-9.9 and 0...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Durdagi S,Korkmaz N,Işık S,Vullo D,Astley D,Ekinci D,Salmas RE,Senturk M,Supuran CT

更新日期：2016-12-01 00:00:00

abstract：:Synthesis and pharmacological evaluation of various 2-(4-isobutylphenyl)propanoic acid derivatives containing 1,3,4-thiadiazole and thiadiazolo[3,2-a][1,3,5]triazine-5-thione nucleus is reported here. The structures of new compounds are supported by IR, (1)H & (13)C NMR data. These compounds were tested in vivo for th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Raval JP,Gandhi AN,Akhaja TN,Myangar KN,Patel NH

更新日期：2012-02-01 00:00:00

abstract：:A series of eighteen pyrrolo[3,2-c]pyridine derivatives were tested for inhibitory effect against FMS kinase. Compounds 1e and 1r were the most potent among all the other tested analogues (IC50 = 60 nM and 30 nM, respectively). They were 1.6 and 3.2 times, respectively, more potent than our lead compound, KIST101029 (...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： El-Gamal MI,Oh CH

更新日期：2018-12-01 00:00:00

abstract：:A new series of 12 N(4)-substituted isatin-3-thiosemicarbazones 2a-l has been synthesized, characterized and screened for in vitro cytotoxic, phytotoxic and urease inhibitory effects. All the compounds proved to be active in the brine shrimp bioassay; 2a, 2b, 2d, 2f and 2h-l exhibited a high degree of cytotoxic activi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pervez H,Chohan ZH,Ramzan M,Nasim FU,Khan KM

更新日期：2009-04-01 00:00:00

abstract：:The present study shows the chemical profile and the in vitro properties (antioxidant and inhibition of nitric oxide production) of the Origanum heracleoticum L. (Lamiaceae). The ethanolic extract of the aerial parts is characterized by terpenes and fatty acids. The extract, with high total phenol and flavonoid conten...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Conforti F,Marrelli M,Menichini F,Tundis R,Statti GA,Solimene U,Menichini F

更新日期：2011-06-01 00:00:00

abstract：:The sequence of human urotensin II (UII) has been recently established as H-Glu-Thr-Pro-Asp-Cys-Phe-Trp-Lys-Tyr-Cys-Val-OH, and it has been reported that UII is the most potent mammalian vasoconstrictor peptide identified so far. A series of UII analogues was synthesized, and the contractile activity of each compound ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Labarrère P,Chatenet D,Leprince J,Marionneau C,Loirand G,Tonon MC,Dubessy C,Scalbert E,Pfeiffer B,Renard P,Calas B,Pacaud P,Vaudry H

更新日期：2003-04-01 00:00:00