Synthesis of some quinazolinones inspired from the natural alkaloid L-norephedrine as EGFR inhibitors and radiosensitizers.

abstract：:The inhibitory effects of a naturally occurring diterpenoid furanolactone, columbin, on partially purified acidic phospholipase A2 (PLA2) from Naja nigricolis was investigated. Columbin inhibited the N. nigricolis PLA2 in a dose related pattern with an IC50 value of 2.5 microM. Double reciprocal plots of initial veloc...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Nok AJ,Balogun E,Lori JA,Abubakar MS

更新日期：2002-02-01 00:00:00

abstract：:HIV entry within the cell involves the presence of at least two chemokine co-receptors, the CCR5 and CXCR4 receptors. Viral entry can be inhibited by the natural ligands for CXCR4, the CXC chemokine SDF-1 and CCR5, the CC chemokines RANTES, MIP-1alpha and MIP-1beta, respectively. Much research has been devoted ultimat...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Scozzafava A,Mastrolorenzo A,Supuran CT

更新日期：2002-04-01 00:00:00

abstract：:Structure-based drug design methods were used to search for novel inhibitors of herpes simplex virus type 1 (HSV-1) thymidine kinase and Mycobacterium tuberculosis thymidylate kinase. The method involved the use of crystal structure complexes to guide database searching for potential inhibitors. A number of weak inhib...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Manallack DT,Pitt WR,Herdewijn P,Balzarini J,De Clercq E,Sanderson MR,Sohi M,Wien F,Munier-Lehmann H,Haouz A,Delarue M

更新日期：2002-06-01 00:00:00

abstract：:The derivatization of racemic 5-[(2-methylphenoxy)methyl]-2-amino-2-oxazoline, developed as an imidazoline binding sites ligand, with (+)-(R)-alpha-methylbenzyl isocyanate was performed in chloroform. The reaction led to two pairs of diastereomers, which were separated by RP-HPLC. A kinetic study of the derivatization...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Matoga M,Forfar I,Chaimbault C,Guillon J,Péhourcq F,Bosc JJ,Rettori MC,Jarry C

更新日期：2002-12-01 00:00:00

abstract：:The protein kinase C (PKC) family of isoenzymes mediate a wide range of signal transduction pathways in many different cells lines. Little is known regarding the presence and functional roles of PKC in Leishmania spp. Here we report the inhibition of parasite PKC by new imidazolidinone compounds. The most active deriv...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Alvarez N,Robledo S,Velez ID,Robert JM,Le Baut G,Le Pape P

更新日期：2002-12-01 00:00:00

abstract：:Rhus coriaria L. (Anacardiaceae) is a well-known spice in the Middle-East and grown in the Central and East Anatolia region of Turkey. A methanolic extract (water-soluble part constituents) of R. coriaria, was found to be an uncompetitive inhibitor of xanthine oxidase and scavenger of superoxide radical in vitro with ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Candan F

更新日期：2003-02-01 00:00:00

abstract：:The quinoline chromophore has long formed the basis for the clinical development of novel antitumour agents. Camptothecin derivatives have already proved their clinical efficacy and compounds such as ascididemin (pyridoacridine family), DHDMC (protoberberine family) have a very promising future. During our search for ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chackal S,Houssin R,Pommery N,Henichart JP

更新日期：2003-04-01 00:00:00

abstract：:Expected for their ability to inhibit HIV replication, four heterodimers with a Nucleoside Reverse Transcriptase Inhibitor (NRTI) and a Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) bound by a linker arm were designed and synthesized. For the NRTIs, d4U, d2U, d4T and 5'-O-acetyl-5-(3-hydroxypropynyl)d2U were ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sugeac E,Fossey C,Ladurée D,Schmidt S,Laumond G,Aubertin AM

更新日期：2003-04-01 00:00:00

abstract：:The inhibitory effects of human alpha2-macroglobulin (alpha2-M), a major plasma proteinase inhibitor, on human pepsin and gastricsin were investigated. The activities of pepsin and gastricsin towards a protein substrate (reduced and carboxymethylated ribonuclease A) were significantly inhibited by alpha2-M at pH 5.5, ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Athauda SB,Nishigai M,Arakawa H,Ikai A,Ukai M,Takahashi K

更新日期：2003-06-01 00:00:00

abstract：:Digitalis compounds are used in the treatment of congestive heart failure as positive inotropic agents; their action is mainly due to the inhibition of Na(+),K(+)-ATPase. A well-known drawback is their arrhythmogenic potential. Attempts to find safer digitalis-like compounds by means of molecular simplifications of th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cerri A,Gobbini M

更新日期：2003-08-01 00:00:00

abstract：:The in vitro and in vivo inhibitory effects of 5-(3alpha, 12alpha-dihydroxy-5-beta-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (1), 5-(3alpha, 7alpha, 12alpha-trihydroxy-5-beta-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (2), 5-(3alpha, 7alpha, 12alpha-triacetoxy-5-beta-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bülbül M,Hisar O,Beydemir S,Ciftçi M,Küfrevioğlu OI

更新日期：2003-08-01 00:00:00

abstract：:Leishmania amazonensis, L. braziliensis and L. chagasi promastigotes were grown in the presence of L-arginine analogs such as Nomega-nitro-L-arginine methyl ester (L-NAME), NG-nitro-L-arginine (L-NNA) and D-arginine (an inactive L-arginine isomer), besides an intracellular calcium chelator [ethylene glycol-bis (beta-a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Genestra M,Cysne-Finkelstein L,Guedes-Silva D,Leon LL

更新日期：2003-10-01 00:00:00

abstract：:Several indole esters were tested as inhibitors of tyrosine kinase p60(c-Src). Compound (4) was found fairly active against the enzyme with IC50 = 1.34 microM. DOCK methodology was used to asses our inhibitors for their inhibitory potency against tyrosine kinase. The docking results showed that compounds (4), (25) and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Olgen S,Akaho E,Nebioglu D

更新日期：2003-12-01 00:00:00

abstract：:In the present study, blood samples from 1183 children aged 0.5-6 years were taken. Three children were found with G6PD deficiency by examining the enzyme activity and hemoglobin ratio. Some kinetic properties of glucose 6-phosphate dehydrogenase enzyme (G6PD) were studied after the purification of the enzyme with amm...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozmen I,Ciftçi M,Küfrevioğlu OI,Curük MA

更新日期：2004-02-01 00:00:00

abstract：:A novel reaction of cytochrome-c from the horse heart with the enzyme glucose oxidase from Aspergillus niger (EC 1.1.3.4), in acidic media is described. Glucose oxidase is able to induce a rapid, profound and irreversible physico-chemical change in cytochrome-c, under anaerobic conditions and in the presence of glucos...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Leskovac V,Trivić S,Pericin D,Kandrac J

更新日期：2004-04-01 00:00:00

abstract：:The villus cavity cells, a specific cell type of the chick chorioallantoic membrane, express both cytosolic carbonic anhydrase in their cytoplasm and HCO3(-)/Cl(-) anion exchangers at their basolateral membranes. By immunohistochemical analysis, we show here that villus cavity cells specifically react with antibodies ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gabrielli MG

更新日期：2004-06-01 00:00:00

abstract：:Two new bi-pyridine compounds, [1,4'] Bipiperidinyl-1'-yl-naphthan-2-yl-methanone (I) and [1,4'] Bipiperidinyl-1'-yl-4-methylphenyl-methane (II) were synthesized and examined for inhibition of the catecholase activity of mushroom tyrosinase in 10 mM phosphate buffer pH 6.8, at 293 K using UV spectrophotometry. Inhibit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Karbassi F,Saboury AA,Khan MT,Choudhary MI,Saifi ZS

更新日期：2004-08-01 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) study has been made on a new series of digitalis-like Na+,K+-ATPase inhibitors in which the guanylhydrazone group has been replaced by an aminoalkyloxime group. The correlations obtained have shown that the oxime moiety, primary amine group, overall size, and polar...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gupta SP,Bagaria P,Kumaran S

更新日期：2004-10-01 00:00:00

abstract：:The synthesis of benzo[c]phenanthridine alkaloid derivatives is described. In vitro antiviral activity against herpes simplex type 1 (HSV1) has been investigated. Contrary to the natural product fagaronine, which did not have any activity in the HSV1 antiviral tests, four 12-alkoxy derivatives showed good activity dem...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vanquelef E,Amoros M,Boustie J,Lynch MA,Waigh RD,Duval O

更新日期：2004-12-01 00:00:00

abstract：:Fifteen new thieno[2,3-b ]- and thieno[3,4-b]pyrrolizines were synthesized and tested against two protein kinases, CDK1/cyclin B and GSK-3. Among these compounds, 3-(3-hydroxy-4-methoxyphenyl)-8H-thieno[2,3-b]pyrrolizin-8-one 4g was identified as a moderate inhibitor of these kinases. Its molecular modeling study brou...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rochais C,Lescot E,Lisowski V,Lepailleur A,Santos JS,Bureau R,Dallemagne P,Meijer L,Rault S

更新日期：2004-12-01 00:00:00

abstract：:The effects of low molecular weight plasma inhibitors from rainbow trout (Oncorhynchus mykiss) (RT) were investigated on the carbonic anhydrase enzyme (CA) activities in in vitro human and in in vivo Sprague-Dawley rat erythrocytes. The RT blood was used as extracellular fluid (plasma) source and plasma inhibitors wer...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hisar O,Beydemir S,Gülçin I,Küfrevioğlu OI,Supuran CT

更新日期：2005-02-01 00:00:00

abstract：:Effects of nicotine, nicotine + vitamin E and nicotine + Hippophea rhamnoides L. extract (HRe-1) on muscle, heart, lungs, testicle, kidney, stomach, brain and liver carbonic anhydrase (CA; EC 4.2.1.1.) enzyme activities were investigated in vivo. Groups of rats were given nicotine (0.5 mg/kg/day, i.p.), nicotine + vit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ciftçi M,Bülbül M,Gül M,Gümüştekin K,Dane S,Süleyman H

更新日期：2005-02-01 00:00:00

abstract：:The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and new antimycobacterial compound development. For this purpose, new alkylsulfanyltriazoles were synthesized and evaluated for antituberculosis activity. The reaction of thienyl-2-aceti...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kaplancikli ZA,Turan-Zitouni G,Chevallet P

更新日期：2005-04-01 00:00:00

abstract：:In vitro as well as in vivo evaluation of the reactivating efficacy of various oximes against nerve agent-inhibited acetylcholinesterase has been usually done with the help of animal experiments. Nevertheless, previously published data indicate that the reactivation potency of oximes may be different in human and anim...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kuca K,Cabal J,Kassa J

更新日期：2005-06-01 00:00:00

abstract：:Polyphenol oxidase (PPO) of nettle (Urtica dioica L.) was extracted and purified through (NH4)2SO4 precipitation, dialysis, and CM-Sephadex ion-exchange chromatography and was used for its characterization. The PPO showed activity to catechol, 4-methylcatechol, L-3,4-dihydroxyphenylalanine (L-DOPA), L-tyrosine, p-cres...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güllçin I,Küfrevioğlu OI,Oktay M

更新日期：2005-06-01 00:00:00

abstract：:Inhibition of cholinesterases (ChE) has been widely used as an environmental biomarker of exposure to organophosphates (OP) and carbamate (CB) pesticides. Different ChE isoforms may be present in the same tissue and may present distinct sensitivities towards environmental contaminants. The present work characterises t...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Nunes B,Carvalho F,Guilhermino L

更新日期：2005-08-01 00:00:00

abstract：:Given the importance of protein phosphorylation in the context of cellular functions, abnormal protein phosphatase activity has been implicated in several diseases, including cancer. These critical roles of protein phosphatases qualify them as potential targets for the development of medicinal compounds that possess d...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bromberg N,Justo GZ,Haun M,Durán N,Ferreira CV

更新日期：2005-10-01 00:00:00

abstract：:Novel 1,3,9-triazacyclopenta[b]fluorene-4,10-diones and 1,3,9-triazacyclopenta[b]fluorene, analogue of ellipticine, were synthesised, and evaluated in vitro for their antiproliferative activity on various breast cancer cell lines. ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Desforges G,Picot L,Montagne C,Thiéry V,Besson T,Joseph B

更新日期：2005-12-01 00:00:00

abstract：:The ability of phosphoramidates Me2NP(O)(Cl)(p-NHC6H4NO2) 1, Me2NP(O)(p-NHC6H4NO2)2 2, (CH3C6H4O-p)P(O)(p-NHC6H4NO2)2 3 and (CH3C6H40-p)2P(O)(p-NHC6H4NO2) 4 to inhibit human acetylcholinesterase (hAChE) has been evaluated by a modified Ellman's method and spectrophotometric measurements. Results showed that compounds ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gholivand K,Shariatinia Z,Khajeh K,Naderimanesh H

更新日期：2006-02-01 00:00:00

abstract：:Isonicotinoylhydrazide Schiff's bases formed by the reaction of substituted and unsubstituted furyl-2-carboxaldehyde and thiophene-2-carboxaldehyde with isoniazid and, their Co (II), Cu (II), Ni (II) and Zn (II) complexes have been synthesized, characterized and screened for their in vitro antibacterial activity again...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Arif M,Shafiq Z,Yaqub M,Supuran CT

更新日期：2006-02-01 00:00:00