Relative binding affinity of novel steroids to androgen receptors in hamster prostate.

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：:Usually, all newborns demonstrate high serum unconjugated bilirubin (UCB) level. UCB may induce adverse effects in the central nervous system. We aimed to evaluate the cytotoxic effects of UCB and the protective effects of docosahexaenoic acid (DHA) on astrocyte cell cultures. The viability of astrocyte cells decrease...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Becerir C,Kılıç İ,Sahin Ö,Özdemir Ö,Tokgün O,Özdemir B,Akca H

更新日期：2013-08-01 00:00:00

abstract：:Neurodegenerative disorders are consequences of progressive and irreversible loss of neurons due to unwanted apoptosis which involves caspases, a group of cysteine proteases that cleave other proteins and inactivate them. Among several different groups of caspase enzymes, caspases-3 plays a key role in apoptosis and a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sharma S,Ravichandran V,Jain PK,Mourya VK,Agrawal RK

更新日期：2008-06-01 00:00:00

abstract：:A recombinant carbonic anhydrase (CA, EC 4.2.1.1) from the soil-dwelling bacterium Enterobacter sp. B13 was cloned and purified by Co(2+) affinity chromatography. Bioinformatic analysis showed that the new enzyme (denominated here B13-CA) belongs to the β-class CAs and to possess 95% homology with the ortholog enzyme ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Eminoğlu A,Vullo D,Aşık A,Çolak DN,Supuran CT,Çanakçı S,Osman Beldüz A

更新日期：2016-12-01 00:00:00

abstract：:[60]Fullerene-peptides represent a simple yet chemically diverse example of a bio-nano conjugate. The C60 moiety provides the following attributes to the conjugate: (a) precise three-dimensional architecture, (b) a large hydrophobic mass and (c) unique electronic properties. Conversely, the peptide component provides:...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Barron AR

更新日期：2016-01-01 00:00:00

abstract：: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 inhibi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zengin Kurt B,Sonmez F,Durdagi S,Aksoydan B,Ekhteiari Salmas R,Angeli A,Kucukislamoglu M,Supuran CT

更新日期：2017-12-01 00:00:00

abstract：:Adenosine receptors have been considered as potential targets for drug development, but one of the main obstacles to this goal is to selectively inhibit one receptor subtype over the others. This subject is particularly crucial for adenosine A2b receptor antagonists (AdoRA2B). The structure–activity relationships of x...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Paz OS,Brito CC,Castilho MS

更新日期：2014-08-01 00:00:00

abstract：:A series of Co(II), Ni(II) and Cu(II) complexes have been synthesized by template condensation of 2,6-diformyl-4-methylphenol and 3-substituted-4-amino-5-hydrazino-1,2,4-triazole with CoCl(2).6H(2)O, NiCl(2).6H(2)O and CuCl(2).2H(2)O chlorides in 2 + 2+2 molar ratio in ethanol. These complexes were characterized by el...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Avaji PG,Patil SA

更新日期：2009-02-01 00:00:00

abstract：:A large number of novel secondary sulfonamides based on the open saccharin scaffold were synthesized and evaluated as selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). They were obtained by reductive ring opening of the newly synthesized N-alkylated saccha...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： D'Ascenzio M,Guglielmi P,Carradori S,Secci D,Florio R,Mollica A,Ceruso M,Akdemir A,Sobolev AP,Supuran CT

更新日期：2017-12-01 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：: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：: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

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

abstract：:Structural modifications around 8-HETE (8-hydroxyeicosatetraenoic acid), a natural agonist of the PPAR (peroxisome proliferator-activated receptor) nuclear receptors have led previously to the identification of a promising analog, the quinoline S 70655. Series of novel quinoline or benzoquinoline derivatives were desi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Liutkus M,Caijo F,Girard AL,Ayral E,Audinot V,Boutin JA,Renard P,Caignard DH,Dacquet C,Ktorza A,Mosset P,Grée R

更新日期：2010-10-01 00:00:00

abstract：:Coumarin, a naturally occurring or synthesised phytochemical, displays a wide range of biological activities. However, chromen-2-ones fused with 1,3-benzoxazine rings is not well documented and there is a gap in the literature which required engaging. The substituted-2-thioxo-chromen-oxazine linear compounds 14a-i and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morrison R,Al-Rawi JM

更新日期：2016-01-01 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：: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：:In this article the synthesis of new 1H-(2'-pyridyl)-3-methyl-5-hydroxypyrazole and 1H-(2'-pyridyl)-3-phenyl-5-hydroxypyrazole complexes with palladium(II) ions is reported. The structures of obtained compounds have been characterized by X-ray crystallography and DFT (density functional theory) calculations. The cytot...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ciolkowski M,Paneth P,Lorenz IP,Mayer P,Rozalski M,Krajewska U,Budzisz E

更新日期：2009-12-01 00:00:00

abstract：:Protein phosphatases are signalling molecules that regulate a variety of fundamental cellular processes including cell growth, metabolism and apoptosis. The aim of this work was to correlate the cytotoxicity of pervanadate and okadaic acid on HL60 cells and their effect on the phosphatase obtained from these cells. Th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Freire AC,Aoyama H,Haun M,Ferreira CV

更新日期：2003-10-01 00:00:00

abstract：:An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newl...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mohamed MI,Zaky HT,Kandile NG

更新日期：2013-12-01 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：:Nerve agents such as sarin, cyclosarin and tabun are organophosphorus substances able to inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators and anticholinergics are generally used as antidotes in the case of intoxication with these agents. None of the known AChE reactivators is able to react...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hrabinova M,Musilek K,Jun D,Kuca K

更新日期：2006-10-01 00:00:00

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

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

abstract：:This study investigates the effect of three new platinum complexes: Pt2(2,4-dimethylpyridine)4(berenil)2 (Pt14), Pt2(3,4-dimethylpyridine)4(berenil)2 (Pt15) and Pt2(3,5-dimethylpyridine)4(berenil)2 (Pt16) on growth and viability of breast cancer cells and their putative mechanism(s) of cytotoxicity. Cytotoxicity was m...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Czarnomysy R,Bielawski K,Muszynska A,Bielawska A,Gornowicz A

更新日期：2016-01-01 00:00:00

abstract：:Direct interaction between 7-chloro-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and primary α-amino acids (exemplified by glycine, alanine, and l-valine) in aqueous ethanolic NaHCO(3) at 70-80°C for 24-72 h produced the respective N-(4-oxoquinolin-7-yl)-α-amino acids (6a-c). The latter ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Al-Hiari YM,Shakya AK,Alzweiri MH,Al-Qirim TM,Shattat G,El-Abadelah MM

更新日期：2011-10-01 00:00:00

abstract：:New hydrazone ligands (HL) derived from 5-substituted isatins and 1-(4-(2-methoxybenzyl)-6-arylpyridazin-3-yl)hydrazines and its complexes with Co(II) and Cu(II) were synthesized. The new hydrazones and their complexes were characterized by means of elemental, spectral analyses and magnetic studies. Primary cytotoxici...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kandile NG,Mohamed MI,Ismaeel HM

更新日期：2012-06-01 00:00:00

abstract：:In the presence of the anionic surfactant sodium n-dodecyl sulphate (SDS), horseradish peroxidase (HRP) undergoes a deactivation process. Suicide inactivation of horseradish peroxidase by hydrogen peroxide(3 mM) was monitored by the absorbance change in product formation in the catalytic reaction cycle. The progress c...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Nazari K,Mahmoudi A,Shahrooz M,Khodafarin R,Moosavi-Movahedi AA

更新日期：2005-06-01 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：: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

abstract：:Histidinol dehydrogenase (HDH, EC EC1.1.1.23) catalyses the final step in the biosynthesis of histidine and constitutes an attractive novel target for the development of new agents against the pathogenous, bacteria Brucella suis. A small library of new HDH inhibitors based on the L-histidinylphenylsulfonyl hydrazide s...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abdo MR,Joseph P,Boigegrain RA,Montero JL,Köhler S,Winum JY

更新日期：2008-06-01 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