听力与言语-语言病理学

行为科学

医学伦理学

你正在浏览JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY期刊下所有文献
  • Bioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation.

    abstract::A series of bio-organometallic-hydrazones of the general formula [{(η5-C5H4)-C(R)=N-N(H)-C6H4-4-SO2NH2}]MLn(MLn = Re(CO)3, Mn(CO)3, FeCp; R=H, CH3) were prepared by reaction of formyl/acetyl organometallic precursors with 4-hydrazino-benzenesulphonamide. All compounds were characterized by conventional spectroscopic t...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1724995

    authors: Brichet J,Arancibia R,Berrino E,Supuran CT

    更新日期:2020-12-01 00:00:00

  • Design, synthesis, and antiprotozoal evaluation of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives.

    abstract::A series of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline, and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives was designed, synthesised, and evaluated in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani, a...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1706502

    authors: Guillon J,Cohen A,Boudot C,Valle A,Milano V,Das RN,Guédin A,Moreau S,Ronga L,Savrimoutou S,Demourgues M,Reviriego E,Rubio S,Ferriez S,Agnamey P,Pauc C,Moukha S,Dozolme P,Nascimento SD,Laumaillé P,Bouchut A,Azas

    更新日期:2020-12-01 00:00:00

  • Coumarins from Magydaris pastinacea as inhibitors of the tumour-associated carbonic anhydrases IX and XII: isolation, biological studies and in silico evaluation.

    abstract::In an in vitro screening for human carbonic anhydrase (hCA) inhibiting agents from higher plants, the petroleum ether and ethyl acetate extracts of Magydaris pastinacea seeds selectively inhibited hCA IX and hCA XII isoforms. The phytochemical investigation of the extracts led to the isolation of ten linear furocoumar...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1713114

    authors: Fois B,Distinto S,Meleddu R,Deplano S,Maccioni E,Floris C,Rosa A,Nieddu M,Caboni P,Sissi C,Angeli A,Supuran CT,Cottiglia F

    更新日期:2020-12-01 00:00:00

  • Synthesis, activity and mechanism of alkoxy-, carbamato-, sulfonamido-, thioureido-, and ureido-derivatives of 2,4,5-trimethylpyridin-3-ol against inflammatory bowel disease.

    abstract::Inflammatory bowel disease (IBD) is a chronic immuno-inflammation in gastrointestinal tract. We have evaluated the activity of the compounds to inhibit the adhesion of monocytes to colon epithelial cells is triggered by a pro-inflammatory cytokine, tumour necrosis factor (TNF)-α. The in vitro activity of the compounds...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1677637

    authors: Chaudhary CL,Gurung P,Jang S,Banskota S,Nam TG,Kim JA,Jeong BS

    更新日期:2020-12-01 00:00:00

  • Discovery of 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives as a novel selective inhibitor scaffold of JNK3.

    abstract::3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives were designed and synthesised as selective inhibitors of JNK3, a target for the treatment of neurodegenerative diseases. Following previous studies, we have designed JNK3 inhibitors to reduce the molecular weight and successfully identified a lead compound that exhibi...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1705294

    authors: Oh Y,Jang M,Cho H,Yang S,Im D,Moon H,Hah JM

    更新日期:2020-12-01 00:00:00

  • Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety.

    abstract::Histamine H3 receptors (H3R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H3R antagonists/inverse agonists have been designed and synthesised via hybriding the H3R pharmacophore (aliphatic amine with propyloxy chain) with the 1,2,4-triazol...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1774573

    authors: Song M,Yan R,Zhang Y,Guo D,Zhou N,Deng X

    更新日期:2020-12-01 00:00:00

  • Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties.

    abstract::A series of compounds incorporating 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl) benzenesulfonamide moieties were synthesised and their chemical structure was confirmed by physico-chemical methods. Carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the compounds were evaluated against human isoforms hCA I an...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1700240

    authors: Bilginer S,Gonder B,Gul HI,Kaya R,Gulcin I,Anil B,Supuran CT

    更新日期:2020-12-01 00:00:00

  • Biochemical and structural characterisation of a protozoan beta-carbonic anhydrase from Trichomonas vaginalis.

    abstract::We report the biochemical and structural characterisation of a beta-carbonic anhydrase (β-CA) from Trichomonas vaginalis, a unicellular parasite responsible for one of the world's leading sexually transmitted infections, trichomoniasis. CAs are ubiquitous metalloenzymes belonging to eight evolutionarily divergent grou...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1774572

    authors: Urbański LJ,Di Fiore A,Azizi L,Hytönen VP,Kuuslahti M,Buonanno M,Monti SM,Angeli A,Zolfaghari Emameh R,Supuran CT,De Simone G,Parkkila S

    更新日期:2020-12-01 00:00:00

  • In vivo antiaging effects of alkaline water supplementation.

    abstract::Telomeres length and telomerase activity are currently considered aging molecular stigmata. Water is a major requirement for our body and water should be alkaline. Recent reports have shown that aging is related to a reduced water intake. We wanted to investigate the effect of the daily intake of alkaline water on the...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1733547

    authors: Logozzi M,Mizzoni D,Di Raimo R,Andreotti M,Macchia D,Spada M,Fais S

    更新日期:2020-12-01 00:00:00

  • Unveiling the interaction profile of rosmarinic acid and its bioactive substructures with serum albumin.

    abstract::Rosmarinic acid, a phytochemical compound, bears diverse pharmaceutical profile. It is composed by two building blocks: caffeic acid and a salvianic acid unit. The interaction profile, responsible for the delivery of rosmarinic acid and its two substructure components by serum albumin remains unexplored. To unveil thi...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1740923

    authors: Papaemmanouil C,Chatziathanasiadou MV,Chatzigiannis C,Chontzopoulou E,Mavromoustakos T,Grdadolnik SG,Tzakos AG

    更新日期:2020-12-01 00:00:00

  • Strong inhibitory activities and action modes of lipopeptides on lipase.

    abstract::Lipopeptides have been reported to exhibit anti-obesity effects. In this study, we obtained a Bacillus velezensis strain FJAT-52631 that could coproduce iturins, fengycins, and surfactins. Results showed that the FJAT-52631 crude lipopeptide, purified fengycin, iturin, and surfactin standards exhibited strong inhibiti...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1734798

    authors: Chen MC,Liu TT,Wang JP,Chen YP,Chen QX,Zhu YJ,Liu B

    更新日期:2020-12-01 00:00:00

  • Synthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells.

    abstract::Novel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 µg/mL for all com...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1755670

    authors: Özdemir Z,Utku S,Mathew B,Carradori S,Orlando G,Di Simone S,Alagöz MA,Özçelik AB,Uysal M,Ferrante C

    更新日期:2020-12-01 00:00:00

  • Enzyme-assisted modification of flavonoids from Matricaria chamomilla: antioxidant activity and inhibitory effect on digestive enzymes.

    abstract::Matricaria chamomilla L. contains antioxidant flavonoids that can have their bioactivity enhanced by enzymatic hydrolysis of specific glycosyl groups. This study implements an untargeted metabolomics approach based on ultra-performance liquid chromatography coupled with electrospray ionisation quadrupole time-of-fligh...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1681989

    authors: Franco EPD,Contesini FJ,Lima da Silva B,Alves de Piloto Fernandes AM,Wielewski Leme C,Gonçalves Cirino JP,Bueno Campos PR,de Oliveira Carvalho P

    更新日期:2020-12-01 00:00:00

  • Design, synthesis, and evaluation of 1, 4-benzodioxan-substituted chalcones as selective and reversible inhibitors of human monoamine oxidase B.

    abstract::The inhibition of monoamine oxidase B (MAO-B) could be an effective approach for the treatment of various neurological disorders. In this study, a series of 1, 4-benzodioxan-substituted chalcone derivatives were designed, synthesised and evaluated for their inhibitory activity against human MAO-B (hMAO-B). The majorit...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2020.1797711

    authors: Kong Z,Sun D,Jiang Y,Hu Y

    更新日期:2020-12-01 00:00:00

  • Probing the role of an invariant active site His in family GH1 β-glycosidases.

    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

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1608198

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

    更新日期:2019-12-01 00:00:00

  • Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors.

    abstract::Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes that are involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel series of benzenesulfonamides incorporating un/substituted ethyl quinoline-3-carboxylate moieties. The newly synthesised compounds were in vitro evaluat...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1652282

    authors: Al-Sanea MM,Elkamhawy A,Paik S,Bua S,Ha Lee S,Abdelgawad MA,Roh EJ,Eldehna WM,Supuran CT

    更新日期:2019-12-01 00:00:00

  • Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3.

    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

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1530223

    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

  • New flavonoid - N,N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer´s disease endowed with neurogenic properties.

    abstract::The design of multi-target directed ligands (MTDLs) is a valid approach for obtaining effective drugs for complex pathologies. MTDLs that combine neuro-repair properties and block the first steps of neurotoxic cascades could be the so long wanted remedies to treat neurodegenerative diseases (NDs). By linking two privi...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1581184

    authors: Estrada-Valencia M,Herrera-Arozamena C,Pérez C,Viña D,Morales-García JA,Pérez-Castillo A,Ramos E,Romero A,Laurini E,Pricl S,Rodríguez-Franco MI

    更新日期:2019-12-01 00:00:00

  • Design, synthesis, molecular modelling, and biological evaluation of novel substituted pyrimidine derivatives as potential anticancer agents for hepatocellular carcinoma.

    abstract::New anticancer agents are highly needed to overcome cancer cell resistance. A novel series of pyrimidine pyrazoline-anthracene derivatives (PPADs) (4a-t) were designed and synthesised. The anti-liver cancer activity of all compounds was screened in vitro against two hepatocellular carcinoma (HCC) cell lines (HepG2 and...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1612889

    authors: Ahmed NM,Youns M,Soltan MK,Said AM

    更新日期:2019-12-01 00:00:00

  • Soyasaponins from Zolfino bean as aldose reductase differential inhibitors.

    abstract::Seven triterpenoid saponins were identified in methanolic extracts of seeds of the Zolfino bean landrace (Phaseolus vulgaris L.) by HPLC fractionation, revealing their ability to inhibit highly purified human recombinant aldose reductase (hAKR1B1). Six of these compounds were associated by MS analysis with the followi...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1553166

    authors: Balestri F,De Leo M,Sorce C,Cappiello M,Quattrini L,Moschini R,Pineschi C,Braca A,La Motta C,Da Settimo F,Del-Corso A,Mura U

    更新日期:2019-12-01 00:00:00

  • Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors.

    abstract::Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites an...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1550752

    authors: Brito CCB,Silva HVCD,Brondani DJ,Faria AR,Ximenes RM,Silva IMD,Albuquerque JFC,Castilho MS

    更新日期:2019-12-01 00:00:00

  • Synthesis, molecular modelling and anticancer evaluation of new pyrrolo[1,2-b]pyridazine and pyrrolo[2,1-a]phthalazine derivatives.

    abstract::Two new series of heterocyclic derivatives with potential anticancer activity, in which a pyrrolo[1,2-b]pyridazine or a pyrrolo[2,1-a]phthalazine moiety was introduced in place of the 3'-hydroxy-4'-methoxyphenyl ring of phenstatin have been synthesised and their structure-activity relationship (SAR) was studied. Fourt...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1550085

    authors: Popovici L,Amarandi RM,Mangalagiu II,Mangalagiu V,Danac R

    更新日期:2019-12-01 00:00:00

  • The first activation study of the β-carbonic anhydrases from the pathogenic bacteria Brucella suis and Francisella tularensis with amines and amino acids.

    abstract::The activation of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacteria Brucella suis and Francisella tularensis with amine and amino acids was investigated. BsuCA 1 was sensitive to activation with amino acids and amines, whereas FtuCA was not. The most effective BsuCA 1 activators were L-adrenaline and...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1630617

    authors: Angeli A,Del Prete S,Pinteala M,Maier SS,Donald WA,Simionescu BC,Capasso C,Supuran CT

    更新日期:2019-12-01 00:00:00

  • Exploration of the residues modulating the catalytic features of human carbonic anhydrase XIII by a site-specific mutagenesis approach.

    abstract::Carbonic anhydrases (CAs) are ubiquitous metallo-enzymes that catalyse the reversible hydration of carbon dioxide to bicarbonate and proton. In humans there are 15 isoforms among which only 12 are catalytically active. Since active human (h) CAs show different efficiency, the understanding of the molecular determinant...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1653290

    authors: De Simone G,Di Fiore A,Truppo E,Langella E,Vullo D,Supuran CT,Monti SM

    更新日期:2019-12-01 00:00:00

  • Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers.

    abstract::A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT ...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1518957

    authors: Wang C,Xu S,Peng L,Zhang B,Zhang H,Hu Y,Zheng P,Zhu W

    更新日期:2019-12-01 00:00:00

  • Synthesis of novel 6,7-dimethoxy-4-anilinoquinolines as potent c-Met inhibitors.

    abstract::HGF/c-Met signalling pathway plays an important role in the development of cancers. A series of 6,7-dimethoxy-4-anilinoquinolines possessing benzimidazole moiety were synthesised and identified as potent inhibitors of the tyrosine kinase c-Met. Their in vitro biological activities against three cancer cell lines (A549...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1533822

    authors: Zhang QW,Ye ZD,Shen C,Tie HX,Wang L,Shi L

    更新日期:2019-12-01 00:00:00

  • Discovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hopping.

    abstract::The bromodomain and extra-terminal (BET) bromodomains, particularly BRD4, have been identified as promising therapeutic targets in the treatment of many human disorders such as cancer, inflammation, obesity, and cardiovascular disease. Recently, the discovery of novel BRD4 inhibitors has garnered substantial interest....

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1587417

    authors: Zhang Z,Gu L,Wang B,Huang W,Zhang Y,Ma Z,Zeng S,Shen Z

    更新日期:2019-12-01 00:00:00

  • Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer's disease therapy.

    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

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1545766

    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

  • Novel 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activity.

    abstract::To develop multifunctional aldose reductase (AKR1B1) inhibitors for anti-diabetic complications, a novel series of 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives were designed and synthesised. Most of the derivatives were found to be potent and selective against AKR1B1, and 2-(7-chloro-2-(3,5-dihydroxyphenoxy)-3-...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1643336

    authors: Hao X,Qi G,Ma H,Zhu C,Han Z

    更新日期:2019-12-01 00:00:00

  • Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1.

    abstract::17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as potential 17β-HSD1 inhibitors have been synthesized. In addition, in...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2019.1634064

    authors: Herman BE,Kiss A,Wölfling J,Mernyák E,Szécsi M,Schneider G

    更新日期:2019-12-01 00:00:00

  • Hyperbaric oxygen therapy ameliorates osteonecrosis in patients by modulating inflammation and oxidative stress.

    abstract::Early stages of avascular necrosis of the femoral head (AVNFH) can be conservatively treated with hyperbaric oxygen therapy (HBOT). This study investigated how HBOT modulates inflammatory markers and reactive oxygen species (ROS) in patients with AVNFH. Twenty-three male patients were treated with two cycles of HBOT, ...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1485149

    authors: Bosco G,Vezzani G,Mrakic Sposta S,Rizzato A,Enten G,Abou-Samra A,Malacrida S,Quartesan S,Vezzoli A,Camporesi E

    更新日期:2018-12-01 00:00:00

  • Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents.

    abstract::To identify anticancer agents with high potency and low toxicity, a series of (Z)-styrylbenzene derivatives were synthesised and evaluated for anticancer activities using a panel of nine cancer cell lines and two noncancerous cell lines. Most derivatives exhibited significant anti-proliferative activities against five...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1513925

    authors: Xin YB,Li JJ,Zhang HJ,Ma J,Liu X,Gong GH,Tian YS

    更新日期:2018-12-01 00:00:00

  • Newer human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2) inhibitors as potential anticancer agents.

    abstract::Human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2), being an age-old target, has attracted attention recently for anticancer drug development. Mycophenolic acid (MPA), a well-known immunosuppressant drug, was used a lead structure to design and develop modestly potent and selective analogues. The steep structure...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1474211

    authors: Shah CP,Kharkar PS

    更新日期:2018-12-01 00:00:00

  • Sulfonamide inhibition studies of two β-carbonic anhydrases from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2.

    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

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1425687

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

    更新日期:2018-12-01 00:00:00

  • Small molecule KDM4s inhibitors as anti-cancer agents.

    abstract::Histone demethylation is a vital process in epigenetic regulation of gene expression. A number of histone demethylases are present to control the methylated states of histone. Among these enzymes, KDM4s are one subfamily of JmjC KDMs and play important roles in both normal and cancer cells. The discovery of KDM4s inhi...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1455676

    authors: Lin H,Li Q,Li Q,Zhu J,Gu K,Jiang X,Hu Q,Feng F,Qu W,Chen Y,Sun H

    更新日期:2018-12-01 00:00:00

  • CAIX furthers tumour progression in the hypoxic tumour microenvironment of esophageal carcinoma and is a possible therapeutic target.

    abstract::The hypoxic tumour microenvironment of solid tumours represents an important starting point for modulating progression and metastatic spread. Carbonic anhydrase IX (CAIX) is a known HIF-1α-dependent key player in maintaining cell pH conditions under hypoxia. We show that CAIX is strongly expressed in esophageal carcin...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1475369

    authors: Drenckhan A,Freytag M,Supuran CT,Sauter G,Izbicki JR,Gros SJ

    更新日期:2018-12-01 00:00:00

  • Pyrrolo[3,2-c]pyridine derivatives with potential inhibitory effect against FMS kinase: in vitro biological studies.

    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

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1491563

    authors: El-Gamal MI,Oh CH

    更新日期:2018-12-01 00:00:00

  • Biochemical characterisation of a Kunitz-type inhibitor from Tamarindus indica L. seeds and its efficacy in reducing plasma leptin in an experimental model of obesity.

    abstract::A trypsin inhibitor isolated from tamarind seed (TTI) has satietogenic effects in animals, increasing the cholecystokinin (CCK) in eutrophy and reducing leptin in obesity. We purified TTI (pTTI), characterised, and observed its effect upon CCK and leptin in obese Wistar rats. By HPLC, and after amplification of resolu...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2017.1419220

    authors: Medeiros AF,Costa IS,Carvalho FMC,Kiyota S,Souza BBP,Sifuentes DN,Serquiz RP,Maciel BLL,Uchôa AF,Santos EAD,Morais AHA

    更新日期:2018-12-01 00:00:00

  • Synthesis and cellular bioactivities of novel isoxazole derivatives incorporating an arylpiperazine moiety as anticancer agents.

    abstract::In our endeavour towards the development of effective anticancer therapeutics, a novel series of isoxazole-piperazine hybrids were synthesized and evaluated for their cytotoxic activities against human liver (Huh7 and Mahlavu) and breast (MCF-7) cancer cell lines. Within series, compounds 5l-o showed the most potent c...

    journal_title:Journal of enzyme inhibition and medicinal chemistry

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1504041

    authors: Çalışkan B,Sinoplu E,İbiş K,Akhan Güzelcan E,Çetin Atalay R,Banoglu E

    更新日期:2018-12-01 00:00:00

  • A highly potent and selective inhibitor Roxyl-WL targeting IDO1 promotes immune response against melanoma.

    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

    pub_type: 杂志文章

    doi:10.1080/14756366.2018.1471688

    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

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