Antiproliferative effects of metal complexes of new isatin hydrazones against HCT116, MCF7 and HELA tumour cell lines.

abstract：:In this study, 14 different 2-[(1-methyl-1H-tetrazole-5-yl)thio]-1-(phenyl)ethanone derivatives (1-14) were synthesized. The structures of the obtained compounds were elucidated using IR, (1)H-NMR, (13)C-NMR and FAB(+)-MS spectral data and elemental analyses results. The compounds were screened for their anticandidal ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kaplancikli ZA,Yurttaş L,Özdemir A,Turan-Zitouni G,Işcan G,Akalın G,Abu Mohsen U

更新日期：2014-02-01 00:00:00

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

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

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

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

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

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

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

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

更新日期：2019-12-01 00:00:00

abstract：:Drug resistance has become a major concern in the field of infection management, therefore searching for new antibacterial agents is getting more challenging. Our study presents an optimized and eco-friendly synthesis scheme for a panel of nitroalkenes bearing various functional groups in the aromatic moiety and bromi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Boguszewska-Czubara A,Lapczuk-Krygier A,Rykala K,Biernasiuk A,Wnorowski A,Popiolek L,Maziarka A,Hordyjewska A,Jasiński R

更新日期：2016-12-01 00:00:00

abstract：:Abstract Twenty-three phenolic compounds were isolated from Dioscorea opposita by bioactivity-guided method and their inhibitory effect against pancreatic lipase was evaluated. A total of 15 isolates reduced lipase activity at IC50 values of less than 50 µM and 3,3',5-trihydroxy-2'-methoxybibenzyl showed the highest i...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yang MH,Chin YW,Yoon KD,Kim J

更新日期：2014-02-01 00:00:00

abstract：:During the treatment of tuberculosis infection, oxidative stress due to anti-tubercular drugs may result in tissue inflammation. It was suggested that treatment with antioxidant drugs could be beneficial as an adjunct to anti-tuberculosis drug therapy. Recently our group has shown that several C-glycosides are inhibit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zaro MJ,Bortolotti A,Riafrecha LE,Concellón A,Morbidoni HR,Colinas PA

更新日期：2016-12-01 00:00:00

abstract：:The human polymerase α (pol α) is a promising target for the therapy of cancer e.g. of the skin. The authors recently built a homology model of the active site of human DNA pol α. This 3D model was now used for molecular modelling studies with eight novel analogues of 2-butylanilino-dATP, which is a highly selective n...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zdrazil B,Schwanke A,Schmitz B,Schäfer-Korting M,Höltje HD

更新日期：2011-04-01 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：:Thirty new aryl-pyridazinone-substituted benzenesulphonylurea derivatives (I-XXX) were synthesized and evaluated for their anti-hyperglycaemic activity in glucose-fed hyperglycaemic normal rats. Twenty-three compounds (III-XI, XIV-XVII, XIX-XXIV, XXVI and XXVIII-XXX) showed more or comparable area under the curve (AUC...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yaseen R,Pushpalatha H,Reddy GB,Ismael A,Ahmed A,Dheyaa A,Ovais S,Rathore P,Samim M,Akthar M,Sharma K,Shafi S,Singh S,Javed K

更新日期：2016-12-01 00:00:00

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

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

abstract：:Berberine was investigated as an inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B) in an attempt to explain its anti-hyperglycemic activitiy. The investigation included simulated docking experiments to fit berberine within the binding pocket of h-PTP 1B. Berberine was found to readily fit within the bindin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bustanji Y,Taha MO,Yousef AM,Al-Bakri AG

更新日期：2006-04-01 00:00:00

abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) had six genetically distinct families described to date in various organisms. There are 16 known CA isoforms in humans. Human CA isoenzymes I and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. Acetylcholine esterase (AChE. EC 3.1.1.7) is a hydrolase that hydrolyzes the n...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Taslimi P,Gulcin I,Ozgeris B,Goksu S,Tumer F,Alwasel SH,Supuran CT

更新日期：2016-01-01 00:00:00

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

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

abstract：:Melatonin (N-acetyl-5-methoxytryptamine) is the chief secretory product of the pineal gland and synthesized enzymatically from serotonin (5-hydroxytryptamine). These indoleamine derivatives play an important role in the prevention of oxidative damage. In the present study, DMPD radical scavenging and cupric ion (Cu(2+...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gulçin I

更新日期：2008-12-01 00:00:00

abstract：:The synthesis of new 4-[2-(alkylamino)ethylthio]pyrrolo[1,2-a]quinoxaline derivatives la-1 is described in five or six steps starting from various substituted nitroanilines 2a-e. The bioisostere 5-[2-(alkylamino)ethylthio]pyrrolo[1,2- a]thieno[3,2-e]pyrazine 1m was also prepared. The new derivatives were evaluated as ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vidaillac C,Guillon J,Moreau S,Arpin C,Lagardère A,Larrouture S,Dallemagne P,Caignard DH,Quentin C,Jarry C

更新日期：2007-10-01 00:00:00

abstract：:The α-glucosidase inhibitory activities of bergenin derivatives were evaluated. Bergenin derivatives were synthesized from bergenin which is a characteristic compound of B. ligulata. A new bergenin derivative, 11-O-(3',4'-dimethoxybenzoyl)-bergenin showed the highest potent inhibitory activity among those of bergenin ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kashima Y,Yamaki H,Suzuki T,Miyazawa M

更新日期：2013-12-01 00:00:00

abstract：:Alzheimer's disease is a progressive neurodegenerative illness accounting for approximately 50% of all types of dementia in elderly people. The only symptomatic treatment proven effective to date is the use of cholinesterase inhibitors to augment surviving cholinergic activity. The purpose of this study is to investig...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Suganthy N,Pandian SK,Devi KP

更新日期：2009-06-01 00:00:00

abstract：:The inhibition of two human carbonic anhydrase (HCA, EC 4.2.1.1) isozymes, the cytosolic HCA I and II, with heavy metal salts of Pb(II), Co(II) and Hg(II) has been investigated. Human erythrocyte CA-I isozyme was purified with a specific activity of 920 EUmg(-1) and a yield of 30% and CA-II isozyme was purified with a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ekinci D,Beydemir S,Küfrevioğlu OI

更新日期：2007-12-01 00:00:00

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

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

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：:Complexes of the type [M(pabh)(H2O)Cl], [M(pcbh)(H2O)Cl] and [M(Hpabh)(H2O)2 (SO4)] where, M = Mn(II), Co(II), Ni(II), Cu(II) and Zn(II); Hpabh = p-amino acetophenone benzoyl hydrazone and Hpcbh = p-chloro acetophenone benzoyl hydrazone have been synthesized and characterized with the help of elemental analyses, elect...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Singh VP,Singh S,Katiyar A

更新日期：2009-04-01 00:00:00

abstract：:This work has been focused on testing the influence of two selected Pt(II) complexes cisplatin, Pt(NH₃)₂Cl₂, and [Pt(dach)Cl₂] on the activity of porcine pancreatic phospholipase A₂ (PLA₂). It has been assumed that this enzyme plays a role in carcinogenesis and that it could be a target in the tumour therapy. The resu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Radisavljević M,Kamčeva T,Bugarčić ŽD,Petković M

更新日期：2013-08-01 00:00:00

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

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

abstract：:3,6-Diazaphenothiazines were obtained in cyclization of 3-amino-3'-nitro-2,4'-dipyridinyl sulfide and the reaction of sodium 3-amino-2-pyridinethiolate with 4-chloro-3-nitropyridine followed by alkylation and heteroarylation. The thiazine ring formation ran via the Smiles rearrangement. The structure elucidation was b...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morak-Młodawska B,Pluta K,Latocha M,Suwińska K,Jeleń M,Kuśmierz D

更新日期：2016-12-01 00:00:00

abstract：:Twenty-five new N-[4-(benzothiazole-2-yl)phenyl]acetamide derivatives bearing different heterocyclic ring systems were synthesized using 2-(4-aminophenyl)benzothiazole structure as a pharmacophoric group. Final compounds were screened for their potential antitumor activity in vitro against approximately 60 human tumor...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yurttaş L,Tay F,Demirayak Ş

更新日期：2015-06-01 00:00:00

abstract：:Protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase are important targets to treat obesity and diabetes, due to their deep correlation with insulin and leptin signalling, and glucose regulation. The methanol extract of Paulownia tomentosa fruits showed potent inhibition against both enzymes. Purification of this...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Song YH,Uddin Z,Jin YM,Li Z,Curtis-Long MJ,Kim KD,Cho JK,Park KH

更新日期：2017-12-01 00:00:00

abstract：:Previously, a glycoglycerolipid isolated from marine algae was reported to be a potent and selective inhibitor of the human Myt1 kinase, an enzyme involved in cell cycle regulation with great potential as an anti-cancer target. Based on that report, a lot of research effort has been invested by several working groups ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rohe A,Göllner C,Erdmann F,Sippl W,Schmidt M

更新日期：2015-06-01 00:00:00

abstract：:The discovery of antibiotics as specific and effective drugs against infectious agents has generated the belief that the famous Paul Erlich theory on magic bullet should be applied to cancer as well. However, after around 60 years of failures in finding a magic bullet against cancer, a question appears mandatory: does...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fais S

更新日期：2016-12-01 00:00:00