Synthesis of new thieno[2,3-b]pyridine derivatives as pim-1 inhibitors.

abstract：:In this study, di(2,6-dimethylphenol) (Di-DMP), di(2,6-diisopropylphenol) (Di-DIP, dipropofol) and di(2,6-di-t-butylphenol) (Di-DTP) were synthesized by the reaction of monomeric phenol derivatives with catalytic CuCl(OH). TMEDA and Na2S2O4. Their antioxidant capacity and radical scavenging activity were examined usin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güllçin I,Daştan A

更新日期：2007-12-01 00:00:00

abstract：:Dietary content of phytohormones may potentially influence metabolic processes in animal cells. This study therefore aimed to investigate the effect of two plant growth regulators homobrassinolide (HB) and gibberellic acid (GBA) on the antioxidant defense status and lipid peroxidation level in the tissues of normal an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Muthuraman P,Srikumar K

更新日期：2009-10-01 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：:We investigated the influence of bronchodilating β2-agonists on the activity of human acetylcholinesterase (AChE) and usual, atypical and fluoride-resistant butyrylcholinesterase (BChE). We determined the inhibition potency of racemate and enantiomers of fenoterol as a resorcinol derivative, isoetharine and epinephrin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bosak A,Knežević A,Gazić Smilović I,Šinko G,Kovarik Z

更新日期：2017-12-01 00:00:00

abstract：:This study presents the synthesis and in vitro pharmacological evaluations of novel 2-(4-cyanophenyl amino)-4-(6-bromo-4-quinolinyloxy)-6-piperazinyl (piperidinyl)-1,3,5-triazines. The title compounds were assayed for their in vitro antimicrobial activity against eight bacteria (Staphylococcus aureus, Bacillus cereus,...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Patel RV,Kumari P,Rajani DP,Chikhalia KH

更新日期：2012-06-01 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 antioxidant activity of extracts from Caesalpinia sappan L. (CSL) was studied in vitro by evaluating the total phenolics, measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) and on reactive nitrogen species (RNS), and measuring the inhibitory effect on Cu(2...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lee MJ,Lee HS,Kim H,Yi HS,Park SD,Moon HI,Park WH

更新日期：2010-10-01 00:00:00

abstract：:The galangal (the rhizome of Alpinia officinarum, Hance) is popular in Asia as a traditional herbal medicine. The present study reports that the galangal extract (GE) can potently inhibit fatty-acid synthase (FAS, E.C.2.3.1.85). The inhibition consists of both reversible inhibition with an IC50 value of 1.73 microg dr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Li BH,Tian WX

更新日期：2003-08-01 00:00:00

abstract：:Recently the literature described the binding of Haptoglobin (HP) with ecotin, a fold-specific serine-proteases inhibitor with an anticoagulant profile and produced by Escherichia coli. In this work, we used some in silico and in vitro techniques to evaluate HP 3D-fold and its interaction with wild-type ecotin and two...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sathler PC,Lourenço AL,Miceli LA,Rodrigues CR,Albuquerque MG,Cabral LM,Castro HC

更新日期：2014-04-01 00:00:00

abstract：:In this study, the synthesis and potential enzyme interactions of new Pyrrolo[2,3-d]pyrimidine derivatives along with their inhibitory activity against SFK enzymes such as Fyn, Lyn, Hck, and c-Src were reported. The results indicated that compounds were slightly active of tested SFK enzymes in comparison with PP2 for ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dincer S,Cetin KT,Onay-Besikci A,Ölgen S

更新日期：2013-10-01 00:00:00

abstract：:A new series of 6, 7-dihydroxy-3-(methylphenyl) chromenones, including three new derivatives, i.e. 6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one (OPC); 6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one (MPC); 6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one (PPC) and one previously described, namely 6,7-dihydroxy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Basaran I,Sinan S,Cakir U,Bulut M,Arslan O,Ozensoy O

更新日期：2008-02-01 00:00:00

abstract：:The inhibition of neuraminidase from Clostridium chauvoei (jakari strain) with partially purified methanolic extracts of some plants used in Ethnopharmacological practice was evaluated. Extracts of two medicinal plants, Tamarindus indicus and Combretum fragrans at 100-1000 microg/ml, both significantly reduced the act...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Useh NM,Nok AJ,Ambali SF,Esievo KA

更新日期：2004-08-01 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：: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：:A quantitative structure-activity relationship analysis was conducted on two different series of pyridinylguanidines acting as inhibitors of urokinase-type plasminogen activator using QuaSAR descriptors of molecular modeling software MOE. Multiple linear regression analysis following a stepwise scheme was employed to ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Karthikeyan C,Moorthy NS,Trivedi P

更新日期：2009-02-01 00:00:00

abstract：:The benzimidazole derivative Schiff bases and their copper(II) (Cu(II)) mixed-polypyridyl complexes (1-4) have been synthesized and characterized by the spectral and analytical techniques. DNA binding/cleavage studies indicate a stronger binding capability for the complex 4 which is confirmed by the absorbance, viscom...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Raman N,Selvan A

更新日期：2012-06-01 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：:The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters ofN-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact e...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Aguirre-Alvarado C,Zaragoza-Martínez F,Rodríguez-Páez L,Nogueda B,Baeza I,Wong C

更新日期：2007-04-01 00:00:00

abstract：:Two fractions of rat intestinal alkaline phosphatase (IAP) were detected by Western blot: 168 +/- 6 and 475 +/- 45 kDa. The low molecular weight fraction constitutes 43% of the isolated proteins exhibiting 82% of the enzymatic activity, and a heavier fraction constitutes 57% of the isolated proteins and has 18% of the...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Brun LR,Brance ML,Rigalli A,Puche RC

更新日期：2006-12-01 00:00:00

abstract：:Protein disulphide isomerase (PDI) in the endoplasmic reticulum catalyzes the rearrangement of disulphide bridges during folding of secreted proteins. It binds various molecules that inhibit its activity. But here, we looked for molecules that would potentiate its activity. PDI reductase activity was measured in vitro...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hassan MH,Alvarez E,Cahoreau C,Klett D,Lecompte F,Combarnous Y

更新日期：2011-10-01 00:00:00

abstract：:The ability of a novel bispyridinium oxime K203 to reactivate VX agent-inhibited acetylcholinesterase was compared with the reactivating efficacy of four commonly used oximes (obidoxime, trimedoxime, methoxime, HI-6) using in vivo model. Our results showed that the reactivating efficacy of the oxime HI-6 is higher tha...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kassa J,Zdarova Karasova J,Sepsova V

更新日期：2013-08-01 00:00:00

abstract：:Melatonin (MLT) is a well-known free-radical scavenger, involving in the prevention of cellular damage that can lead to cancer, ageing and a variety of neurodegenerative diseases. Research on MLT-related compounds has been required to optimise the maximum pharmaceutical activity with the lowest side effects. In our on...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shirinzadeh H,Ince E,Westwell AD,Gurer-Orhan H,Suzen S

更新日期：2016-12-01 00:00:00

abstract：:Cytosine deaminase (CD) from Aspergillus parasiticus, which has half-life of 1.10 h at 37°C, was stabilized by immobilization on calcium alginate beads. The immobilized CD had pH and temperature optimum of 5 and 50°C respectively. The immobilized enzyme also stoichiometrically deaminated Cytosine and 5-fluorocytosine ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zanna H,Nok AJ,Ibrahim S,Inuwa HM

更新日期：2013-12-01 00:00:00

abstract：:Phthalates, used in medical devices (MDs), have been identified as reproductive and developmental toxicants. Their toxicity varies somewhat depending on the specific phthalate and is in part linked to the activation of Peroxisome Proliferating-Activated Receptors (PPARs). So, the use of MDs containing targeted phthala...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kambia N,Farce A,Belarbi K,Gressier B,Luyckx M,Chavatte P,Dine T

更新日期：2016-01-01 00:00:00

abstract：CONTEXT:Tumor acidity represents a major cause of chemoresistance. Proton pump inhibitors (PPIs) can neutralize tumor acidity, sensitizing cancer cells to chemotherapy. OBJECTIVE:To compare the anti-tumor efficacy of different PPIs in vitro and in vivo. MATERIALS AND METHODS:In vitro experiments PPIs anti-tumor effic...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lugini L,Federici C,Borghi M,Azzarito T,Marino ML,Cesolini A,Spugnini EP,Fais S

更新日期：2016-08-01 00:00:00

abstract：:Drug target interactions (DTIs) are crucial in pharmacology and drug discovery. Presently, experimental determination of compound-protein interactions remains challenging because of funding investment and difficulties of purifying proteins. In this study, we proposed two in silico models based on support vector machin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shar PA,Tao W,Gao S,Huang C,Li B,Zhang W,Shahen M,Zheng C,Bai Y,Wang Y

更新日期：2016-12-01 00:00:00

abstract：:Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. NFOH has higher activity and lower mutagenicity. The aim of this work was to assess whether NF and its derivative NFOH would also be inhibitors of cruzain, besides their trypanothione reductase inhibitory ac...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Trossini GH,Malvezzi A,T-do Amaral A,Rangel-Yagui CO,Izidoro MA,Cezari MH,Juliano L,Chin CM,Menezes CM,Ferreira EI

更新日期：2010-02-01 00:00:00

abstract：:The synthesis of 1,2-dioxolane derivatives in two different acetophenone series, as simplified models of natural coumarins is described. 2-Acetyl-3-acetoxy-4-(3-hydroperoxy-3-methylbut-1-enyl)phenyl acetate and 2-acetyl-5-acetoxy4-(3-hydroperoxy-3-methylbut-1-enyl) phenyl acetate synthons are used as precursors to the...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Helesbeux JJ,Peyronnet D,Labaïed M,Grellier P,Frappier F,Seraphin D,Richomme P,Duval O

更新日期：2002-12-01 00:00:00

abstract：:Fatty acid synthase (FAS) has been proposed to be a new drug target for the development of anticancer agents because of the significant difference in expression of FAS between normal and tumour cells. Since a n-hexane-soluble extract from Ginkgo biloba was demonstrated to inhibit FAS activity in our preliminary test, ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Oh J,Hwang IH,Hong CE,Lyu SY,Na M

更新日期：2013-06-01 00:00:00

abstract：:The copper(II) complexes of the type [Cu(SPF)(A(n))Cl]/[Cu(PFL)(A(n))Cl] (where SPF is sparfloxacin, PFL is pefloxacin and A(n) is 2,2'-dipyridylamine/pyridine-2-carboxalehyde/thiophene-2-carboxaldehyde) were synthesised and were found to have a pyramidal geometry with a square base. The superoxide dismutase (SOD) lik...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Patel MN,Parmar PA,Gandhi DS

更新日期：2011-04-01 00:00:00