Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers.

abstract：:Monoacylglycerol lipase is a serine hydrolase that plays a major role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol. A wide number of MAGL inhibitors are reported in literature; however, many of them are characterised by an irreversible mechanism of action and this behavior determin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Granchi C,Caligiuri I,Bertelli E,Poli G,Rizzolio F,Macchia M,Martinelli A,Minutolo F,Tuccinardi T

更新日期：2017-12-01 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 series of compounds incorporating 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl) benzenesulfonamide moieties were synthesised and their chemical structure was confirmed by physico-chemical methods. Carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the compounds were evaluated against human isoforms hCA I an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bilginer S,Gonder B,Gul HI,Kaya R,Gulcin I,Anil B,Supuran CT

更新日期：2020-12-01 00:00:00

abstract：:The inhibitory effects of 13-epimeric estrones, D-secooxime and D-secoalcohol estrone compounds on human placental 17β-hydroxysteroid dehydrogenase type 1 isozyme (17β-HSD1) were investigated. The transformation of estrone to 17β-estradiol was studied by an in vitro radiosubstrate incubation method. 13α-Estrone inhibi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Herman BE,Szabó J,Bacsa I,Wölfling J,Schneider G,Bálint M,Hetényi C,Mernyák E,Szécsi M

更新日期：2016-01-01 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：: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：:The inhibition of monoamine oxidase B (MAO-B) could be an effective approach for the treatment of various neurological disorders. In this study, a series of 1, 4-benzodioxan-substituted chalcone derivatives were designed, synthesised and evaluated for their inhibitory activity against human MAO-B (hMAO-B). The majorit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kong Z,Sun D,Jiang Y,Hu Y

更新日期：2020-12-01 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：:Breast cancer is the second most frequent cancer affecting women. Among all endocrine therapies for the treatment of breast cancer, inhibition of estrogen biosynthesis is becoming an interesting complementary approach to the use of antiestrogens. The enzyme type 1 17beta-hydroxysteroid dehydrogenase (17beta-HSD) plays...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tremblay MR,Boivin RP,Luu-The V,Poirier D

更新日期：2005-04-01 00:00:00

abstract：:Several 2,5-disubstituted-1,3,4-oxadiazoles (4a-f) and 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles (7a-f) were synthesized and characterized by elemental analyses and spectral data. These compounds were screened for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. Compo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chawla G,Kumar U,Bawa S,Kumar J

更新日期：2012-10-01 00:00:00

abstract：:Thirty new aryl-pyridazinone-substituted benzenesulphonylurea derivatives (I-XXX) were synthesized and evaluated for their anti-hyperglycaemic activity in glucose-fed hyperglycaemic normal rats. Twenty-three compounds (III-XI, XIV-XVII, XIX-XXIV, XXVI and XXVIII-XXX) showed more or comparable area under the curve (AUC...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yaseen R,Pushpalatha H,Reddy GB,Ismael A,Ahmed A,Dheyaa A,Ovais S,Rathore P,Samim M,Akthar M,Sharma K,Shafi S,Singh S,Javed K

更新日期：2016-12-01 00:00:00

abstract：:Drug resistance has become a major concern in the field of infection management, therefore searching for new antibacterial agents is getting more challenging. Our study presents an optimized and eco-friendly synthesis scheme for a panel of nitroalkenes bearing various functional groups in the aromatic moiety and bromi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Boguszewska-Czubara A,Lapczuk-Krygier A,Rykala K,Biernasiuk A,Wnorowski A,Popiolek L,Maziarka A,Hordyjewska A,Jasiński R

更新日期：2016-12-01 00:00:00

abstract：:The whole plants of Carpesium genus are used in traditional medicine as anti-pyretic, analgesic and vermifugic, including a topical application for sores and inflammation. A previous study on Carpesium genus suggested that the antiplasmodial activity against Plasmodium falciparum was due to the existence of 11(13)- de...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kim JJ,Chung IM,Jung JC,Kim MY,Moon HI

更新日期：2009-02-01 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：: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

abstract：:Histone demethylation is a vital process in epigenetic regulation of gene expression. A number of histone demethylases are present to control the methylated states of histone. Among these enzymes, KDM4s are one subfamily of JmjC KDMs and play important roles in both normal and cancer cells. The discovery of KDM4s inhi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lin H,Li Q,Li Q,Zhu J,Gu K,Jiang X,Hu Q,Feng F,Qu W,Chen Y,Sun H

更新日期：2018-12-01 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：: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：: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：:The reaction mechanism of glycoside hydrolases belonging to family 1 (GH1) of carbohydrate-active enzymes classification, hydrolysing β-O-glycosidic bonds, is well characterised. This family includes several thousands of enzymes with more than 20 different EC numbers depending on the sugar glycone recognised as substr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Strazzulli A,Perugino G,Mazzone M,Rossi M,Withers SG,Moracci M

更新日期：2019-12-01 00:00:00

abstract：:Previous investigations into the binding of substrates/cofactors to the PAH active site have only concentrated on Phe, thienylalanine and BH(4). This is the first reported investigation to model aliphatic thioether amino acid substrates to PAH. The clearance of the thioether substrates (4.82-79.09% of Phe) in the rat ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Patel NG,Iliadou C,Boonyapiwat B,Barlow DJ,Forbes B,Mitchell SC,Steventon GB

更新日期：2008-12-01 00:00:00

abstract：:Fraxamoside, a macrocyclic secoiridoid glucoside featuring a hydroxytyrosol group, was recently identified as a xanthine oxidase inhibitor (XOI) comparable in potency in vitro to the standard antigout drug allopurinol. However, this activity and its considerably higher value than its derivatives oleuropein, oleoside 1...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vitale RM,Antenucci L,Gavagnin M,Raimo G,Amodeo P

更新日期：2017-12-01 00:00:00

abstract：:The copper(II) complexes of the type [Cu(SPF)(A(n))Cl]/[Cu(PFL)(A(n))Cl] (where SPF is sparfloxacin, PFL is pefloxacin and A(n) is 2,2'-dipyridylamine/pyridine-2-carboxalehyde/thiophene-2-carboxaldehyde) were synthesised and were found to have a pyramidal geometry with a square base. The superoxide dismutase (SOD) lik...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Patel MN,Parmar PA,Gandhi DS

更新日期：2011-04-01 00:00:00

abstract：:Melatonin (N-acetyl-5-methoxytryptamine) is the chief secretory product of the pineal gland and synthesized enzymatically from serotonin (5-hydroxytryptamine). These indoleamine derivatives play an important role in the prevention of oxidative damage. In the present study, DMPD radical scavenging and cupric ion (Cu(2+...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gulçin I

更新日期：2008-12-01 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：: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：:Dietary content of phytohormones may potentially influence metabolic processes in animal cells. This study therefore aimed to investigate the effect of two plant growth regulators homobrassinolide (HB) and gibberellic acid (GBA) on the antioxidant defense status and lipid peroxidation level in the tissues of normal an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Muthuraman P,Srikumar K

更新日期：2009-10-01 00:00:00

abstract：:In this study, di(2,6-dimethylphenol) (Di-DMP), di(2,6-diisopropylphenol) (Di-DIP, dipropofol) and di(2,6-di-t-butylphenol) (Di-DTP) were synthesized by the reaction of monomeric phenol derivatives with catalytic CuCl(OH). TMEDA and Na2S2O4. Their antioxidant capacity and radical scavenging activity were examined usin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güllçin I,Daştan A

更新日期：2007-12-01 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：:C3 and C4 plant carbonic anhydrases (CAs) are zinc-enzymes that catalyze the reversible hydration of CO2. They are sub-divided in three classes: α, β and γ, being distributed between both photosynthetic subtypes. The C4 dicotyledon species Flaveria bidentis (L.) "Kuntze" contains a small gene family encoding three dis...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dathan NA,Alterio V,Troiano E,Vullo D,Ludwig M,De Simone G,Supuran CT,Monti SM

更新日期：2014-08-01 00:00:00