Synthesis of functionalized amino acid derivatives as new pharmacophores for designing anticancer agents.

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：:A series of 2-chloro-quinoline-based imidazopyridines 6a-l and imidazothiazoles 6m-o bearing a bulky alkylamine side chain were synthesized as soybean 15-LOX inhibitors. The target compounds 6a-o were prepared via one-pot reaction of 2-chloroquinoline-3-carbaldehyde (3), heteroaromatic amidine 4, and alkyl isocyanides...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dianat S,Moghimi S,Mahdavi M,Nadri H,Moradi A,Firoozpour L,Emami S,Mouradzadegun A,Shafiee A,Foroumadi A

更新日期：2016-01-01 00:00:00

abstract：:Exposure of the N-methoxycarbonyl-bicyclic-keto-acid 5 (improved preparation) to the Barnick beta-keto-acid synthesis yielded an aqueous solution of the sodium salts of the beta-keto-acids 26 and 27 which on heating at 60-65 degrees C furnished the N-methoxycarbonyl-tricyclic-ketone 9 (55%) plus the hydroxy-ketone 28 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bowman MA,Bowman RE,Davies RV,Haran G,Harris PJ,Smith HJ,Steele RW,Walker N,Whiting K

更新日期：2002-06-01 00:00:00

abstract：:A series of benzoic acid derivatives 1-10 have been synthesised by two different methods. Compounds 1-6 were synthesised by a facile procedure for esterification using N,N'-dicyclohexylcarbodiimide (DCC) as a coupling agent, methylene chloride as a solvent system and dimethylaminopyridine (DMAP). While 7-10 were synth...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Khan SB,Hassan Khan MT,Jang ES,Akhtar K,Seo J,Han H

更新日期：2010-12-01 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：: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：:The mechanism of inhalation anesthesia remains to be fully elucidated. While certain neuronal membrane proteins are considered sites of action, cytosolic proteins may also be targets. We hypothesize that inhaled anesthetics may act via glyceraldehyde 3-phosphate dehydrogenase (GAPDH), which has recently been shown to ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Swearengin TA,Fibuch EE,Seidler NW

更新日期：2006-10-01 00:00:00

abstract：:Identification of a new class of antitumor agent capable to induce apoptosis without triggering necrotic cell death event is challenging. The present communication describes the multicomponent synthesis of seven new (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-dithiocarbamates and their in vitro antiproliferative activity o...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Laskar S,Sánchez-Sánchez L,López-Ortiz M,López-Muñoz H,Escobar-Sánchez ML,Sánchez AT,Regla I

更新日期：2017-12-01 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：: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：:An efficient and economical synthesis of some new fluorine substituted phthalides was accomplished from two γ-keto acids, 2-(4-fluorobenzoyl)benzoic acid and 2-(3,5-dinitro-4-flurobenzoyl)benzoic acid. Each acid was reacted with various phenolic compounds in presence of catalytic quantity of concentrated sulphuric aci...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chamoli T,Rawat MS,Jacob M

更新日期：2012-10-01 00:00:00

abstract：:An array of novel spiro imidazolidine derivatives was synthesized in dry media and was screened for their anti-microbial activities. Structure-activity relationship results revealed that compounds 22, 23 against P.aeruginosa, 24 against S.aureus, 24, 25 against K.pneumonia, 27 against S.aureus, β-H.streptococcus, 29 a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kanagarajan V,Thanusu J,Gopalakrishnan M

更新日期：2011-04-01 00:00:00

abstract：:A novel series of substituted pyrimidine compounds bearing N-phenylpyrazole and terminating with aryl and cyclic sulfonamido moiety were designed, synthesized, and evaluated in vitro as antiproliferative agents against a panel of 53 cell lines of different tissues at the NCI. Among them, compound 1d with p-chlorobenze...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gamal El-Din MM,El-Gamal MI,Abdel-Maksoud MS,Yoo KH,Baek D,Choi J,Lee H,Oh CH

更新日期：2016-01-01 00:00:00

abstract：:The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was c...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gökçe B,Gençer N,Arslan O,Turkoğlu SA,Alper M,Köçkar F

更新日期：2012-02-01 00:00:00

abstract：:The synthesis and biological evaluation of some novel thiazolofluorenones, thiazolofluorenes and thiazoloanthraquinones, substituted with amino side-chains are described. These polyheterocyclic compounds have been synthesized via the corresponding imino-1,2,3-dithiazoles. Their cytotoxic activity and their eventual se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chabane H,Pierre A,Leonce S,Pfeiffer B,Renard P,Thiery V,Guillaumet G,Besson T

更新日期：2004-12-01 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：:Two new series of heterocyclic derivatives with potential anticancer activity, in which a pyrrolo[1,2-b]pyridazine or a pyrrolo[2,1-a]phthalazine moiety was introduced in place of the 3'-hydroxy-4'-methoxyphenyl ring of phenstatin have been synthesised and their structure-activity relationship (SAR) was studied. Fourt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Popovici L,Amarandi RM,Mangalagiu II,Mangalagiu V,Danac R

更新日期：2019-12-01 00:00:00

abstract：:Adult male ICR mice were treated by intraperitoneal injection with 250 mg/kg of bodyweight of commercial malathion (a dose corresponding to 1/12 the LD50). After 6 h, acetylcholinesterase (AChE) activity in blood, liver, and six brain regions was determined. A statistically significant inhibition was observed in whole...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Banasik M,Stedeford T,Persad AS,Ueda K,Tanaka S,Muro-Cacho C,Harbison RD

更新日期：2003-12-01 00:00:00

abstract：:Flavonoids, polyphenolic phytochemicals, are ubiquitous in plants and are commonly present in the human diet. They may exert diverse beneficial effects, including antioxidant and anticarcinogenic activities. The present study was designed to evaluate three biomolecules that play important roles in the apoptotic proces...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： de Sousa RR,Queiroz KC,Souza AC,Gurgueira SA,Augusto AC,Miranda MA,Peppelenbosch MP,Ferreira CV,Aoyama H

更新日期：2007-08-01 00:00:00

abstract：CONTEXT:Bacterial sphingomyelinase (SMase) is thought to play a crucial role in bacterial evasion of the immune response during the early stages of infections. OBJECTIVE:The objective of this study was to predict the chemical structure required for competitive SMase inhibition, then synthesize and test the effect of p...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Oda M,Imagawa H,Kato R,Yabiku K,Yoshikawa T,Takemoto T,Takahashi H,Yamamoto H,Nishizawa M,Sakurai J,Nagahama M

更新日期：2014-06-01 00:00:00

abstract：:Microbial resistance to the available drugs poses a serious threat in modern medicine. We report the design, synthesis and in vitro antimicrobial evaluation of new functionalized 2,3-dihydrothiazoles and 4-thiazolidinones tagged with sulfisoxazole moiety. Compound 8d was most active against Bacillis subtilis (MIC, 0.0...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Nasr T,Bondock S,Eid S

更新日期：2016-01-01 00:00:00

abstract：:A new series of tertiary amine derivatives of chlorochalcone (4a∼4l) were designed, synthesized and evaluated for the effect on acetylcholinesterase (AChE) and buthylcholinesterase (BuChE). The results indicated that all compounds revealed moderate or potent inhibitory activity against AChE, and some possessed high se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gao XH,Zhou C,Liu HR,Liu LB,Tang JJ,Xia XH

更新日期：2017-12-01 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：:In the present study, some thiazole derivatives were synthesized via the ring closure reaction of 1-[2-(2-oxobenzo[d]thiazol-3(2H)-yl)acetyl]thiosemicarbazide with various phenacyl bromides. The chemical structures of the compounds were elucidated by (1)H NMR, (13)C NMR and mass spectral data and elemental analyses. E...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Turan-Zitouni G,Ozdemir A,Kaplancikli ZA,Altintop MD,Temel HE,Çiftçi GA

更新日期：2013-06-01 00:00:00

abstract：:The synthesis, in vitro antimicrobial activities of some novel hydroxy pyridines supported with various pharmacophores is described. Twenty-six out of the tested 58 compounds exhibited variable inhibitory effects on the growth of the tested Gram positive and Gram negative bacteria. The tested compounds revealed better...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Faidallah HM,Rostom SA,Khan KA,Basaif SA

更新日期：2013-10-01 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：:In this work, we reported the synthesis and evaluation of antibacterial and antifungal activities of three new compound series obtained from 6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazole-3-acetic acid hydrazide: 2-{[6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl}-N-alkyl/arylhydrazinecarbothioamides (2a-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güzeldemirci NU,Satana D,Küçükbasmacı O

更新日期：2013-10-01 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：:A new series of N-heteroarylsubstituted triazolosulfonamide compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. Compounds (3 a-k) were prepared by propargylation of N-heteroaryl compounds. Compound 5 was obtained from sulfanilamide...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Balci A,Arslan M,Nixha AR,Bilen C,Ergun A,Gençer N

更新日期：2015-06-01 00:00:00

abstract：:Sulfonamide-bearing thiazole compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of the 12 syn...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kılıcaslan S,Arslan M,Ruya Z,Bilen Ç,Ergün A,Gençer N,Arslan O

更新日期：2016-12-01 00:00:00