Synthesis and cytotoxic activity of thiazolofluorenone derivatives.

abstract：:The results of extensive quantitative structure-activity relationship (QSAR) analyses on 15 series of cytochrome P450 inhibitors, covering a total of 7 enzymes and 199 compounds, are reported. In general, it is found that lipophilicity represents the most important single factor in describing differences in inhibitory...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lewis DF,Lake BG,Dickins M

更新日期：2007-02-01 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：:In mammalian skin, melanocyte proliferation and melanogenesis can be stimulated by keratinocytes, fibroblasts and other regulatory factors. To determine whether hydroxybenzyl alcohols (HBAs) show more inhibitory in melanocytes cultured alone or in melanocytes co-cultured with keratinocytes, we developed a murine melan...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Liu SH,Chu IM,Pan IH

更新日期：2008-08-01 00:00:00

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：:Lipopeptides have been reported to exhibit anti-obesity effects. In this study, we obtained a Bacillus velezensis strain FJAT-52631 that could coproduce iturins, fengycins, and surfactins. Results showed that the FJAT-52631 crude lipopeptide, purified fengycin, iturin, and surfactin standards exhibited strong inhibiti...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chen MC,Liu TT,Wang JP,Chen YP,Chen QX,Zhu YJ,Liu B

更新日期：2020-12-01 00:00:00

abstract：:Trypanothione reductase (TR) is a major enzyme in trypanosomatids. Its substrate, trypanothione is a molecule containing a tripeptide (L-glutamic acid-cysteine-glycine) coupled to a polyamine, spermidine. This redox system (TR/Trypanothione) is vital for parasite survival within the host cell and has been described as...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Castro-Pinto DB,Lima EL,Cunha AS,Genestra M,De Léo RM,Monteiro F,Leon LL

更新日期：2007-02-01 00:00:00

abstract：:A series of eighteen pyrrolo[3,2-c]pyridine derivatives were tested for inhibitory effect against FMS kinase. Compounds 1e and 1r were the most potent among all the other tested analogues (IC50 = 60 nM and 30 nM, respectively). They were 1.6 and 3.2 times, respectively, more potent than our lead compound, KIST101029 (...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： El-Gamal MI,Oh CH

更新日期：2018-12-01 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

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：:In this study, firstly, antioxidant and polyphenol oxidase (PPO) properties of Yomra apple were investigated. Seventeen phenolic constituents were measured by reverse phase-high-performance liquid chromatography (RP-HPLC). Total phenolic compounds (TPCs), ferric reducing antioxidant power (FRAP) and 2, 2-diphenyl-1-pi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Can Z,Dincer B,Sahin H,Baltas N,Yildiz O,Kolayli S

更新日期：2014-12-01 00:00:00

abstract：:The two β-carbonic anhydrases (CAs, EC 4.2.1.1) recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 aromatic, heterocyclic, and aliphatic sulfonamides and one sulfamate, many of which are clinically used agents. CAS1 was ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vullo D,Lehneck R,Pöggeler S,Supuran CT

更新日期：2018-12-01 00:00:00

abstract：:Serum paraoxonase (PON1) is a high-density lipoprotein (HDL)-associated enzyme that protects lipoproteins, both low-density lipoprotein (LDL) and HDL, against oxidation, and is considered as an antioxidative/anti-inflammatory component of HDL. In this study, PON1 was purified from bovine serum by ammonium sulfate prec...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sayın M,Guler OO

更新日期：2015-02-01 00:00:00

abstract：:This paper reports the synthesis of O-methyl and O-ethyl NSAID hydroxamic acids, their antimicrobial activities, and their ability to inhibit urease and soybean lipoxygenase activities. Ibuprofen and fenoprofen hydroxamic acids with free hydroxy groups present the highest antimicrobial activity, while indomethacin and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rajić Z,Perković I,Butula I,Zorc B,Hadjipavlou-Litina D,Pontiki E,Pepeljnjak S,Kosalec I

更新日期：2009-10-01 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：:Three series of sintenin derivatives (compounds 1-14) were designed and prepared and their antioxidative and neuroprotective effects were evaluated. The in vitro models of scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, chelating ferrous ions, inhibiting the rat brain homogenates lipid peroxidation, and prot...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yang LX,Zhang LJ,Huang KX,Kun Li X,Hu LH,Wang XY,Stockigt J,Zhao Y

更新日期：2009-04-01 00:00:00

abstract：:A set of novel quinolone-triazole conjugates (12-31) were synthesized in three steps in good yields starting from 2-phenylquinoline-4-carboxylic acid. All the intermediates, as well as the final 1,2,4-triazolyl quinolines were fully characterized by their detailed spectral analysis utilizing different techniques such ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Verbanac D,Malik R,Chand M,Kushwaha K,Vashist M,Matijašić M,Stepanić V,Perić M,Paljetak HČ,Saso L,Jain SC

更新日期：2016-01-01 00:00:00

abstract：:A series of azatricyclodiones and octahydro-benzo[f]isoindoles have been synthesized by (4+2) Diels-Alder cycloaddition of maleimides with furfuryl amine. Reaction of azatricyclodiones with isocyanates led to the respective ureides. All of the compounds were screened against a number of bacteria and fungi. One of the ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Saxena N,Singh NT,Mishra M,Keshava GB,Shukla PK,Tripathi RP

更新日期：2008-08-01 00:00:00

abstract：:Tetrahydrocannabinol and other mixed cannabinoid (CB) receptors CB(1)/CB(2) receptor agonists are well established to elicit antinociceptive effects and psychomimetic actions, however, their potential for abuse have dampened enthusiasm for their therapeutic development. In an effort to refine a semi-rigid structural f...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Taher AT,Kadry HH,Allarà M,Di Marzo V,Abadi AH,Abouzid KA

更新日期：2013-06-01 00:00:00

abstract：:A series of bio-organometallic-hydrazones of the general formula [{(η5-C5H4)-C(R)=N-N(H)-C6H4-4-SO2NH2}]MLn(MLn = Re(CO)3, Mn(CO)3, FeCp; R=H, CH3) were prepared by reaction of formyl/acetyl organometallic precursors with 4-hydrazino-benzenesulphonamide. All compounds were characterized by conventional spectroscopic t...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Brichet J,Arancibia R,Berrino E,Supuran CT

更新日期：2020-12-01 00:00:00

abstract：:Nineteen 5-nitrothiazolylthiosemicarbazones were synthesized from 5-nitrothiazole by three-step synthesis and evaluated for in vitro activities against seven mycobacterial species. Among them, N-(5-nitro-1, 3-thiazol-2-yl)-2-((Z)-4-[(phenylmethyl)oxy]phenylmethylidene)hydrazine-1-carbothioamide (4m) was found to be th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sriram D,Yogeeswari P,Senthilkumar P,Sangaraju D

更新日期：2010-02-01 00:00:00

abstract：:Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor-2 (VEGFR-2), two protein tyrosine kinases, are involved in pathological disorders and the progression of different types of carcinomas. Concomitant inhibition of both tyrosine kinase activities appears to be an attractive target fo...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Garofalo A,Goossens L,Lemoine A,Farce A,Arlot Y,Depreux P

更新日期：2010-04-01 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：:Indoleamine 2,3-dioxygenase 1 (IDO1) activity links to immune escape of cancers. Inhibition of IDO1 provides a new approach for cancer treatment. Most clinical IDO1 drugs show marginal efficacy as single agents. On basis of molecular docking and pharmacophore modelling, a novel inhibitor Roxyl-WL was discovered with a...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Xu G,Wang T,Li Y,Huang Z,Wang X,Zheng J,Yang S,Fan Y,Xiang R

更新日期：2018-12-01 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：:Berberine was investigated as an inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B) in an attempt to explain its anti-hyperglycemic activitiy. The investigation included simulated docking experiments to fit berberine within the binding pocket of h-PTP 1B. Berberine was found to readily fit within the bindin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bustanji Y,Taha MO,Yousef AM,Al-Bakri AG

更新日期：2006-04-01 00:00:00

abstract：:Direct interaction between 7-chloro-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and primary α-amino acids (exemplified by glycine, alanine, and l-valine) in aqueous ethanolic NaHCO(3) at 70-80°C for 24-72 h produced the respective N-(4-oxoquinolin-7-yl)-α-amino acids (6a-c). The latter ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Al-Hiari YM,Shakya AK,Alzweiri MH,Al-Qirim TM,Shattat G,El-Abadelah MM

更新日期：2011-10-01 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：:In this study, the synthetic way to new N-pyridinyl(methyl)indolylpropanamides acting as non acidic NSAIDs has been described. Pharmacomodulation was carried out at N(1) and C(5) of the indole ring and at the level of the propanamide chain. N(3)-pyridinylmethyl-[1(4-chlorobenzyl-5-chloroindol-3-yl)propanamide represen...

journal_title：Journal of enzyme inhibition and medicinal chemistry

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

更新日期：2008-10-01 00:00:00

abstract：:The activation of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacteria Brucella suis and Francisella tularensis with amine and amino acids was investigated. BsuCA 1 was sensitive to activation with amino acids and amines, whereas FtuCA was not. The most effective BsuCA 1 activators were L-adrenaline and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Angeli A,Del Prete S,Pinteala M,Maier SS,Donald WA,Simionescu BC,Capasso C,Supuran CT

更新日期：2019-12-01 00:00:00

abstract：:The needs for diverse inhibitors of α-glucosidase (α-Gls) encouraged us to synthesize five different poly-hydroxy functionalized pyrimidine-fused heterocyclic (PHPFH) molecules, having either aliphatic or aromatic side chains (C1-C5) and their inhibitory activities were examined spectroscopically against yeast and mou...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yousefi R,Alavian-Mehr MM,Mokhtari F,Panahi F,Mehraban MH,Khalafi-Nezhad A

更新日期：2013-12-01 00:00:00