Small molecule inhibitors of cyclin-dependent kinase 9 for cancer therapy.

abstract：:Incubation of 50 mM D-glucose with aspartate aminotransferase (AST, EC 2.6.1.1) preparations (purified pig heart enzyme or a rat liver 20,000 x g supernatant) at 25 degrees C had no effect on enzyme activity. 50 mM D-fructose or D-ribose gradually inhibited pig heart AST under the same conditions to zero activity afte...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Drsata J,Beránek M,Palicka V

更新日期：2002-02-01 00:00:00

abstract：:2-Amino-1,3,4-thiadiazole undergoes a condensation reaction with furane-, thiophene- and pyrrole-2-carboxaldehyde to form tridentate NNO, NNS and NNN donor Schiff bases. These Schiff bases were further used to obtain complexes of the type [M(L)2]X, where M = Co(II), Cu(II), Ni(II) or Zn(II), L = L1, L2 or L3 and X = C...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Pervez H,Rauf A,Scozzafava A,Supuran CT

更新日期：2002-04-01 00:00:00

abstract：:Bhilawanol diene (3) isolated from bhilawan nut shell liquid was found to be a potent inhibitor of both soybean and potato lipoxygenases with IC50 values of 0.85 microM and 1.1 microM, respectively. However, the monoene (2) and saturated (1) bhilawanols exhibited relatively lower inhibitory activity. In addition, inhi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Nagabhushana KS,Umamaheshwari S,Tocoli FE,Prabhu SK,Green IR,Ramadoss CS

更新日期：2002-08-01 00:00:00

abstract：:A series of novel N-substituted-(indol-2-yl)carboxamides (12-18) and (indol-3-alkyl)carboxamides (25-31) were synthesized and evaluated as inhibitors of the inflammation process. Pharmacomodulation at the level of the amidic nitrogen by incorporation of the previously described pharmacophoric moieties 6-aminolutidine,...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Breteche A,Duflos M,Dassonville A,Nourrisson MR,Brelet J,Le Baut G,Grimaud N,Petit JY

更新日期：2002-12-01 00:00:00

abstract：:A series of (+/-)-3-(4-aminophenyl) pyrrolidin-2,5-diones substituted in the 1-, 3- or 1,3-position with an aryl or long chain alkyl function are weak inhibitors of the metabolism of all-trans retinoic acid (RA) by rat liver microsomes (68-75% inhibition) compared with ketoconazole (85%). Further studies with the 1-cy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kirby AJ,Lelain R,Mason P,Maharlouie F,Nicholls PJ,Smith HJ,Simons C

更新日期：2002-10-01 00:00:00

abstract：:The chemical modifications of rabbit liver carbonyl reductase (RLCR) with phenylglyoxal (PGO) and 2,3,4-trinitrobenzenesulfonate sodium (TNBS), which are respective chemical modifiers of arginine and lysine residues, were examined. RLCR was rapidly inactivated by these modifiers. Kinetic data for the inactivation demo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Imamura Y,Koga T,Shimada H,Otagiri M

更新日期：2003-02-01 00:00:00

abstract：:The syntthesis of new N-propargyl-3-pyrrol-1-ylindanamine derivatives, analogues of rasagiline, is described in ten steps starting from the corresponding arylaldehydes via the corresponding cis-3-pyrrol-1-ylindanamines. The cis-configuration of some intermediates has been established using X-ray analysis and NOE exper...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Guillon J,Hébert G,Dallemagne P,Léger JM,Vidaillac C,Thé C,Lisowski V,Rault S,Demotes-Mainard J,Jarry C

更新日期：2003-04-01 00:00:00

abstract：:The effect of N-isopropyl oxamate on the activity of alpha-hydroxyacid dehydrogenase-isozyme II (HADH-isozyme II) from Trypanosoma cruzi was investigated. The kinetic studies showed that this substance was a competitive inhibitor of this isozyme. The attachment of the nonpolar isopropylic branched chain to the nitroge...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Elizondo S,Chena MA,Rodríguez-Páez L,Nogueda B,Baeza I,Wong C

更新日期：2003-06-01 00:00:00

abstract：:A series of new compounds was obtained by reaction of aromatic/heterocyclic sulfonamides incorporating amino groups with N,N-diphenylcarbamoyl chloride and diphenylacetyl chloride. These sulfonamides were assayed for the inhibition of three carbonic anhydrase (CA, EC 4.2.1.1) isozymes: the cytosolic CA I and CA II, an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Franchi M,Vullo D,Gallori E,Pastorek J,Russo A,Scozzafava A,Pastorekova S,Supuran CT

更新日期：2003-08-01 00:00:00

abstract：:Pyrocatechol was studied as an inhibitor of jack bean urease in 20 mM phosphate buffer, pH 7.0, 25 degrees C. The inhibition was monitored by an incubation procedure in the absence of substrate and reaction progress studies in the presence of substrate. It was found that pyrocatechol acted as a time- and concentration...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kot M,Zaborska W

更新日期：2003-10-01 00:00:00

abstract：:The synthesis of some new aryl acetic acids and amides and a pharmacochemical study and quantitative structure-activity relationships (QSAR) on them are described. The compounds were screened for their biological activity using the carrageenin induced rat paw oedema model and a significant inhibition of oedema occurre...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Michaelidou A,Hadjipavlou-Litina D

更新日期：2003-12-01 00:00:00

abstract：:Xanthine oxidase (XO), an enzyme involved in purine metabolism, is a source of either oxidants (superoxide radical) or antioxidants (uric acid). Interference with XO activity can lead to oxidative stress, thus contributing to the pathogenesis of cardiovascular diseases. The adenosine receptors antagonist, 1,3-dipropyl...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sousa T,Morato M,Fernandes E,Carvalho F,Albino-Teixeira A

更新日期：2004-02-01 00:00:00

abstract：:Some novel cephalexin-derived furanyl, thiophenyl, pyrrolyl, salicylyl and pyridyl Schiff's bases and their cobalt (II), copper (II), nickel (II) and zinc (II) complexes have been synthesized and studied for their antifungal properties against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Pervez H,Khan KM,Rauf A,Maharvi GM,Supuran CT

更新日期：2004-02-01 00:00:00

abstract：:The synthesis of new potential inhibitors of human chymase is described. Treatment of dihydroimidazo[1,5-a]indole and [1,5-b]isoquinoline-dione with thioaryl followed by oxidation gave the N-arylsulfonylmethyl of polycyclic hydantoin derivatives 3, 5 and 6. ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Alagille D,Pfeiffer B,Scalbert E,Ferry G,Boutin JA,Renard P,Viaud-Massuard MC

更新日期：2004-04-01 00:00:00

abstract：:Schiff's bases were obtained from aromatic/heterocyclic sulfonamides and amino-sulfonamide derivatives, such as sulfanilamide, homosulfanilamide, 4-aminoethyl-benzenesulfonamide and 5-amino-1,3,4-thiadiazole-2-sulfonamide. Metal complexes of some of these Schiff's bases, incorporating Zn(II), Co(lI), Ni(II) and Cu(II)...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mahmood-Ul-Hassan,Chohan ZH,Scozzafava A,Supuran CT

更新日期：2004-06-01 00:00:00

abstract：:The reversible phosphorylation of proteins mediates cellular signals in eukaryotic cells. RNA interference inhibits the expression of genes and proteins in a sequence-specific manner and provides a tool to study the functions of target molecules. The effect of RNA interference on protein phosphatase isoforms in HEK-29...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morimoto H,Okamura H,Yoshida K,Kitamura S,Haneji T

更新日期：2004-08-01 00:00:00

abstract：:Black cumin seed, Nigella sativa L., and its oils have traditionally been used for the treatment of asthma and other inflammatory diseases. Thymoquinone (TQ) has been proposed to be one of the major active components of the drug. Since leukotrienes (LTs) are important mediators in asthma and inflammatory processes, th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Mansour M,Tornhamre S

更新日期：2004-10-01 00:00:00

abstract：:The present study was designed to investigate conazoles as new antileishmanial agents. Several 3-imidazolylalkyl-indoles were prepared under mild reaction conditions and pharmacomodulation at N1 and C5 of the indole ring and at the level of the alkyl chain (R) was carried out starting from the corresponding 3-formylin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Na YM,Lebouvier N,Le Borgne M,Pagniez F,Alvarez N,Le Pape P,Le Baut G

更新日期：2004-12-01 00:00:00

abstract：:The present study was designed to follow our pharmacomodulation work in the field of non-steroidal aromatase inhibitors. All target compounds 12a-h and 28a-h were tested in vitro for human placental aromatase inhibition, using testosterone or androstenedione as the substrate for the aromatase enzyme and the IC50 and r...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lézé MP,Le Borgne M,Marchand P,Loquet D,Kogler M,Le Baut G,Palusczak A,Hartmann RW

更新日期：2004-12-01 00:00:00

abstract：:A QSAR analysis for substituted (S)-phenylpiperidines as dopamine (DA) antagonists is described. The studied derivatives differ at the nitrogen substitutent (R) and at the substitutents (X) of the phenyl-ring. The analysis was done using the C-QSAR suite program (Biobyte) through the Internet. Clog P, CMR, M(vol), B1 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pontiki EA,Hadjipavlou-Litina DJ,Demertzis AM,Hadjidakis I,Kovala-Demertzi D

更新日期：2005-02-01 00:00:00

abstract：:Carbonic anhydrase (CA) was purified from four different cell localisation (outer peripheral, cytosolic, inner peripheral and integral) in bovine stomach using affinity chromatography with Sepharose-4B-L-tyrosine sulphanilamide. During the purification steps, the activity of the enzyme was measured using p-nitrophenyl...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Demir Y,Nadaroğlu H,Demir N

更新日期：2005-02-01 00:00:00

abstract：:A series of benzofuran-2-yl-(phenyl)-3-pyridylmethanol derivatives were prepared using an efficient 1-step procedure in good yields. In addition furan-2-yl-(phenyl)-3-pyridylmethanol derivatives were also prepared to determine the effect of the benzene ring in benzofuran with respect to inhibitory activity. The pyridy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Saberi MR,Shah K,Simons C

更新日期：2005-04-01 00:00:00

abstract：:A series of hydrazine derivatives was synthesized in order to evaluate their monoamine oxidase A (MAO-A) inhibitory effects. MAO-A inhibitory activity of 4-tosyl benzoic acid carbohydrazide was quite potent, similarly to that of the corresponding 4-benzyloxy-benzoic acid carbohydrazide and its N-cyanoethylated derivat...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dar A,Khan KM,Ateeq HS,Khan S,Rahat S,Perveen S,Supuran CT

更新日期：2005-06-01 00:00:00

abstract：:A series of substituted 2,4,5-triphenylisothiazol-3(2H)-one 1,1-dioxides 9 was synthesized and investigated as inhibitors of human leukocyte elastase (HLE). All compounds were found to inhibit HLE in a time-dependent manner and most of them exhibited kobs/[I] values > 300M(-1)s(-1). The most potent 3-oxosultam of this...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gütschow M,Pietsch M,Themann A,Fahrig J,Schulze B

更新日期：2005-08-01 00:00:00

abstract：:Nine potential AChE reactivators were synthesized using a modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by insecticide chlorpyrifos was tested in vitro. 2,2'-Bis(hydroxyiminomethyl)-1,1'-(1,4-phenylenedimethyl)-bispyridinium dibromide seems to be the most potent AChE re...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Musilek K,Kuca K,Jun D,Dohnal V,Dolezal M

更新日期：2005-10-01 00:00:00

abstract：:In vitro effects of ketamine and bupivacaine drugs on bovine lactoperoxidase (LPO; E.C. 1.11.1.7) enzyme activity were investigated. Lactoperoxidase was purified with Amberlite CG 50 resin, CM Sephadex C-50 ion-exchange chromatography, and Sephadex G-100 gel filtration chromatography from skimmed bovine milk. Rz(A412/...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozdemir H,Uğuz MT

更新日期：2005-10-01 00:00:00

abstract：:Fifteen compounds derived from the 2(3H)-benzothiazolone template with an acyl side-chain in position-6 were evaluated for their lipid-lowering action in mice. Among these compounds, 6-benzoyl-2(3H)-benzothiazolone was found to be the most potent one both in mice models receiving a hypercholesterolemic diet (for 15 da...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yous S,Lebegue N,Poupaert JH,Chavatte P,Berthelot P

更新日期：2005-12-01 00:00:00

abstract：:Thymidine phosphorylase (EC 2.4.2.4) catalyses the reversible phosphorolysis of pyrimidine 2'-deoxynucleosides, forming 2-deoxyribose-1-phosphate and pyrimidine. 5-Chloro-6-(2-imino-pyrrolidin-1-yl)methyl-uracil hydrochloride (TPI, 1) and its 5-bromo analogue (2), 6-(2-amino-imidazol-1-yl)methyl-5-bromo-uracil (3) and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gbaj A,Edwards PN,Reigan P,Freeman S,Jaffar M,Douglas KT

更新日期：2006-02-01 00:00:00

abstract：:Andrographolide 1, a diterpenoid lactone of the plant Andrographis paniculata, known to possess antitumour activity in in vitro and in vivo breast cancer models was subjected to semisynthesis leading to the preparation of a number of novel compounds. These compounds exhibited in vitro antitumour activity with moderate...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jada SR,Hamzah AS,Lajis NH,Saad MS,Stevens MF,Stanslas J

更新日期：2006-04-01 00:00:00

abstract：:Catalase enzyme (H202: oxidoreductase; E.C. 1.11.1.6) was purified from human skin homogenate using ammonium sulfate precipitation and DEAE-Sephadex A50 ion exchange chromatography at 4 degrees C and some characteristics of the enzyme were investigated. The human skin enzyme, having a specific activity of 1354.5 EU/mg...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Altikat S,Coban A,Ciftci M,Ozdemir H

更新日期：2006-04-01 00:00:00