Small molecule KDM4s inhibitors as anti-cancer agents.

abstract：:Complexes of the type [M(pabh)(H2O)Cl], [M(pcbh)(H2O)Cl] and [M(Hpabh)(H2O)2 (SO4)] where, M = Mn(II), Co(II), Ni(II), Cu(II) and Zn(II); Hpabh = p-amino acetophenone benzoyl hydrazone and Hpcbh = p-chloro acetophenone benzoyl hydrazone have been synthesized and characterized with the help of elemental analyses, elect...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Singh VP,Singh S,Katiyar A

更新日期：2009-04-01 00:00:00

abstract：:Histamine H3 receptors (H3R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H3R antagonists/inverse agonists have been designed and synthesised via hybriding the H3R pharmacophore (aliphatic amine with propyloxy chain) with the 1,2,4-triazol...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Song M,Yan R,Zhang Y,Guo D,Zhou N,Deng X

更新日期：2020-12-01 00:00:00

abstract：:Novel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 µg/mL for all com...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Özdemir Z,Utku S,Mathew B,Carradori S,Orlando G,Di Simone S,Alagöz MA,Özçelik AB,Uysal M,Ferrante C

更新日期：2020-12-01 00:00:00

abstract：:The current study was designed to assess the inhibitory activity of Broussonetia papyrifera-derived polyphenols against 3-chymotrypsin-like and papain-like coronavirus cysteine proteases. The isolated compounds were broussochalcone B (1), broussochalcone A (2), 4-hydroxyisolonchocarpin (3), papyriflavonol A (4), 3'-(3...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Park JY,Yuk HJ,Ryu HW,Lim SH,Kim KS,Park KH,Ryu YB,Lee WS

更新日期：2017-12-01 00:00:00

abstract：:To develop multifunctional aldose reductase (AKR1B1) inhibitors for anti-diabetic complications, a novel series of 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives were designed and synthesised. Most of the derivatives were found to be potent and selective against AKR1B1, and 2-(7-chloro-2-(3,5-dihydroxyphenoxy)-3-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hao X,Qi G,Ma H,Zhu C,Han Z

更新日期：2019-12-01 00:00:00

abstract：:HGF/c-Met signalling pathway plays an important role in the development of cancers. A series of 6,7-dimethoxy-4-anilinoquinolines possessing benzimidazole moiety were synthesised and identified as potent inhibitors of the tyrosine kinase c-Met. Their in vitro biological activities against three cancer cell lines (A549...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zhang QW,Ye ZD,Shen C,Tie HX,Wang L,Shi L

更新日期：2019-12-01 00:00:00

abstract：:The small and highly electronegative fluorine atom can play a remarkable role in medicinal chemistry. Selective installation of fluorine into a therapeutic or diagnostic small molecule candidate can enhance a number of pharmacokinetic and physicochemical properties such as improved metabolic stability and enhanced mem...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shah P,Westwell AD

更新日期：2007-10-01 00:00:00

abstract：:In this study, 5-chloro-3H-spiro-[1,3-benzothiazole-2,3'-indole]-2'(1'H)-one derivatives 3a-l were synthesized by the reaction of 1H-indole-2,3-diones 1a-l with 2-amino-4-chlorothiophenol 2 in ethanol. 3a-l were tested for their abilities to inhibit lipid peroxidation (LP), scavenge DPPH(•) and ABTS(•+) radicals, and ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ermut G,Karalı N,Özsoy N,Can A

更新日期：2014-08-01 00:00:00

abstract：:The inhibitory effect of four structurally related flavonoids, apigenin, baicalein, luteolin and quercetin on the matrix metalloproteinase (MMP)-9 and -13 expressions in osteoblasts was investigated. Treatment with IL-1β induced both MMP-9 and -13 mRNA expressions as measured by quantitative real-time PCR. Luteolin an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yang H,Liu Q,Ahn JH,Kim SB,Kim YC,Sung SH,Hwang BY,Lee MK

更新日期：2012-04-01 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：: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：: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：:Organophosphorus compounds pose a potential threat to both military and civilian populations. Since post-exposure therapy has its limitations, our research was focused on the possibility of improving pretreatment in order to limit the toxic effects of tabun. We determined the protective index of various combinations o...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Berend S,Katalinić M,Vrdoljak AL,Kovarik Z,Kuca K,Radić B

更新日期：2010-08-01 00:00:00

abstract：:Inflammatory bowel disease (IBD) is a chronic immuno-inflammation in gastrointestinal tract. We have evaluated the activity of the compounds to inhibit the adhesion of monocytes to colon epithelial cells is triggered by a pro-inflammatory cytokine, tumour necrosis factor (TNF)-α. The in vitro activity of the compounds...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chaudhary CL,Gurung P,Jang S,Banskota S,Nam TG,Kim JA,Jeong BS

更新日期：2020-12-01 00:00:00

abstract：:Several (thiazol-2-yl)hydrazone derivatives from 2-, 3- and 4-acetylpyridine were synthesized and tested against human monoamine oxidase (hMAO) A and B enzymes. Most of them had an inhibitory effect in the low micromolar/high nanomolar range, being derivatives of 4-acetylpyridine selective hMAO-B inhibitors also at lo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： D'Ascenzio M,Chimenti P,Gidaro MC,De Monte C,De Vita D,Granese A,Scipione L,Di Santo R,Costa G,Alcaro S,Yáñez M,Carradori S

更新日期：2015-12-01 00:00:00

abstract：:The purpose of this study was the evaluation of the xanthine oxidase (XO) inhibition produced by some synthetic 2-styrylchromones. Ten polyhydroxylated derivatives with several substitution patterns were synthesised, and these and a positive control, allopurinol, were tested for their effects on XO activity by measuri...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fernandes E,Carvalho F,Silva AM,Santos CM,Pinto DC,Cavaleiro JA,Bastos Mde L

更新日期：2002-02-01 00:00:00

abstract：:A trypsin inhibitor isolated from tamarind seed (TTI) has satietogenic effects in animals, increasing the cholecystokinin (CCK) in eutrophy and reducing leptin in obesity. We purified TTI (pTTI), characterised, and observed its effect upon CCK and leptin in obese Wistar rats. By HPLC, and after amplification of resolu...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Medeiros AF,Costa IS,Carvalho FMC,Kiyota S,Souza BBP,Sifuentes DN,Serquiz RP,Maciel BLL,Uchôa AF,Santos EAD,Morais AHA

更新日期：2018-12-01 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：:In the present study we have evaluated the antigenotoxic effects of Farnesol (FL) a 15-carbon isoprenoid alcohol against benzo (a) pyrene [B(a)P] (125 mg kg(- 1).b.wt oral) induced toxicity. B(a)P administration lead to significant induction in Cytochrome P450 (CYP) content and aryl hydrocarbon hydrolase (AHH) activit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jahangir T,Sultana S

更新日期：2008-12-01 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：:Starting from a simple general reaction mechanism of activation of aspartic proteinases zymogens involving a uni- and a bimolecular simultaneous activation route and a reversible inhibition step, the time course equation of the zymogen, inhibitor and activated enzyme concentrations have been derived. Likewise, express...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Muñoz-López A,Sotos-Lomas A,Arribas E,Masia-Perez J,Garcia-Molina F,García-Moreno M,Varon R

更新日期：2007-04-01 00:00:00

abstract：:Cobalt (II), copper (II), nickel (II) and zinc (II) complexes with 2-hydroxy-1-naphthaldehyde derived N-substituted sulfonamides have been synthesized and the nature of bonding and structure of compounds have been deduced from physical, analytical and spectral (IR, (1)H NMR, (13)C NMR, Mass and electronic) data. An oc...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chohan ZH,Supuran CT

更新日期：2008-04-01 00:00:00

abstract：:This study aimed to investigate the antidiabetic, antilipidaemic and antioxidant activities of Citrus medica cv Diamante (Rutaceae) hydroalcoholic (CD) peel extract in Zucker diabetic fatty (ZDF) rats. The ability of CD to protect against oxidative stress was investigated by using different in vitro assays and in vivo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Menichini F,Tundis R,Loizzo MR,Bonesi M,D'Angelo D,Lombardi P,Mastellone V

更新日期：2016-12-01 00:00:00

abstract：:Recently we found that 1-methyldodecanoylindole-2-carboxylic acid (1) and 1-[2-(4-carboxyphenoxy)ethyl]-3-dodecanoylindole-2-carboxylic acid (4) were inhibitors of the cytosolic phospholipase A2alpha (cPLA2alpha)-mediated arachidonic acid release in calcium ionophore A23187-stimulated human platelets with IC50-values ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ghasemi A,Elfringhoff AS,Lehr M

更新日期：2005-10-01 00:00:00

abstract：:3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives were designed and synthesised as selective inhibitors of JNK3, a target for the treatment of neurodegenerative diseases. Following previous studies, we have designed JNK3 inhibitors to reduce the molecular weight and successfully identified a lead compound that exhibi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Oh Y,Jang M,Cho H,Yang S,Im D,Moon H,Hah JM

更新日期：2020-12-01 00:00:00

abstract：:EGFR tyrosine kinase has been reported mainly in 40-80% of non-small lung cancers, in addition to colon and breast cancers. In this study, we illustrate the synthesis of a highly potent antitumor agent. The synthesized compound 4 was screened at NCI, USA, for antitumor activity against non-small lung cancer, colon can...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gabr MT,El-Gohary NS,El-Bendary ER,El-Kerdawy MM

更新日期：2015-02-01 00:00:00

abstract：:Analogs of pralidoxime, which is a commercial antidote for intoxication from neurotoxic organophosphorus compounds, were designed, synthesized, characterized, and tested as potential inhibitors or reactivators of acetylcholinesterase (AChE) using the Ellman's test, nuclear magnetic resonance, and molecular modeling. T...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Petronilho Eda C,Rennó Mdo N,Castro NG,da Silva FM,Pinto Ada C,Figueroa-Villar JD

更新日期：2016-12-01 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：: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：CONTEXT:Endocrinological factors have been recently described to affect respiratory mechanics. OBJECTIVE:To review recent literature data, most of all obtained by the end-inflation occlusion method, describing the effects of molecules of endocrinological interest such as endothelin, erythropoietin and renin-angiotensi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rubini A,Frigo A,Carniel EL

更新日期：2016-12-01 00:00:00