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Wyniki wyszukiwania dla: acridine
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Human CYP2 family of cytochrome P-450 takes part in metabolism of two acridine antitumor agents, C-1311 and C-1748, selected for I phase of clinical trials
PublikacjaPraca zawiera wyniki badań metabolicznej transformacji przeciwnowotworowych pochodnych akrydyny wobec zestawu 16 prób enzymów mikrosomalnych, pochodzących z wątroby 16 różnych pacjentów. Wykazano, że za metabolizm tych związków u człowieka odpowiedzialne są głównie izoenzymy z rodziny CYP2.
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9-(tert-Butylamino)acridine. Acta Cryst. E**2002 vol. 58 s. o458-o460, 2rys. 2 tab. bibliogr. 11 poz. 9(tert-Butyloamino)akrydyna.
PublikacjaTytułowy związek występuje w krysztale w aminowej formie tautomerycznej. Re-szta akrydyny jest lekko zgieta wzdłuż linii C9-N10. Orientacja grupy t-bu-tyloaminowej umożliwia sprzężenie pomiędzy parą elektronową azotu aminowegoi elektronami ă pierścienia akrydynowego. W strukturze krystalicznej wystę-puje wiązanie wodorowe pomiędzy atomem azotu pierścienia akrydynowego i eg-zocykliczną grupą NH.
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‘Acridines’ as New Horizons in Antifungal Treatment
PublikacjaFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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Akrydyny jako związki aktywne przeciwnowotworowo = Acridines as antitumor drugs
PublikacjaAkrydyny należą do grupy policyklicznych związków heteroaromatycznych. Wykazują szeroki zakres aktywności biologicznej obejmujący aktywność przeciwpierwotniakową, przeciwbakteryjną,przeciwwirusową i przeciwnowotworową. Pochodne akrydyny o działaniu przeciwnowotworowym wykazują zróżnicowany mechanizm działania na poziomie molekularnym. Z uzyskanych dotychczas danych wynika, że jednym z podstawowych etapów działania jest tworzenie...
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Natural and synthetic acridines/acridones as antitumor agents: their biological activities and methods of synthesis.
PublikacjaPraca stanowi przegląd opisanych w literaturze chemicznej modyfikacji struktur naturalnych i syntetycznych pochodnych akrydyny i akrydonu. Artykuł obejmuje swym zakresem metody syntezy, a także wpływ budowy cząsteczek tych związków na ich aktywność przeciwnowotworową oraz mechanizm działania.
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublikacjaImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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The interactions of monomeric acridines and unsymmetrical bisacridines (UAs) with DNA duplexes: an insight provided by NMR and MD studies
PublikacjaMembers of a novel class of anticancer compounds, exhibiting high antitumor activity, i.e. the unsymmetrical bisacridines (UAs), consist of two heteroaromatic ring systems. One of the ring systems is an imidazoacridinone moiety, with the skeleton identical to the structural base of Symadex. The second one is a 1-nitroacridine moiety, hence it may be regarded as Nitracrine’s structural basis. These monoacridine units are connected...
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublikacjaMany people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. Todate, many acridine/acridone analogues have been obtained,which, inter alia, exhibit...
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2-Methylphenyl 2-methoxyacridine-9-carboxylate
PublikacjaThe title compound, C22H17NO3, crystallizes in the monoclinic space group P21/c with four molecules per unit cell. The molecules are arranged in centrosymmetric pairs, joined via the C and attached H atoms in the meta position relative to the methoxy group. These pairs are bonded in the crystalline phase as a result of non-specific dispersive interactions, and through a network of C—H⋯O interactions involving the non-bonded O...
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10-Methyl- and 9,10-dimethyl acridinium methyl sulfate
PublikacjaThe title compounds, C(14)H(12)N(+).CH(3)O(4)S(-), (I), and C(15)H(14)N(+).CH(3)O(4)S(-), (II), respectively, crystallize with the planar 10-methylacridinium or 9,10-dimethylacridinium cations arranged in layers, parallel to the twofold axis in (I) and perpendicular to the 2(1) axis in (II). Adjacent cations in both compounds are packed in a 'head-to-tail' manner. The methyl sulfate anion only exhibits planar symmetry in (II)....
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublikacjaIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
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Abundance and biomass of bacteria in two Arctic glacial fjords
PublikacjaTotal numbers and biomass of bacterioplankton in water in two glacial fjords off west Spitsbergen have been studied. Samples were collected from different water depth layers - from the surface to 80-90 m. Total bacterial number (TBN), biomass and morphological structure were determined by the acridine orange direct count method. The highest values of TBN and biomass in the water column were found on stations situated adjacent...
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A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance
PublikacjaFungal resistance remains a significant threat and a leading cause of death worldwide. Thus, overcoming microbial infections have again become a serious clinical problem. Although acridine derivatives are widely analyzed as anticancer agents, only a few reports have demonstrated their antifungal activity. In an effort to develop biologically active antifungals, twelve novel C-857 (9-(2′ -hydroxyethylamino)-1-nitroacridine) and...
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublikacjaThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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9-Cyano-10-methylacridinium hydrogen dinitrate
PublikacjaThe title compound, C15H11N2+·HN2O6−, crystallizes in the monoclinic space group C2/c with four molecules in the unit cell. The planar 9-cyano-10-methylacridinium cations lie on crystallographic twofold axes and are arranged in layers, almost perpendicular to the ac plane, in such a way that neighbouring molecules are positioned in a `head-to-tail' manner. These cations and the hydrogen dinitrate anions are linked through C—H⋯O...
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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublikacjaDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...
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The Effect of Conjugation with Octaarginine, a Cell-Penetrating Peptide on Antifungal Activity of Imidazoacridinone Derivative
PublikacjaAcridine cell-penetrating peptide conjugates are an extremely important family of compounds in antitumor chemotherapy. These conjugates are not so widely analysed in antimicrobial therapy, although bioactive peptides could be used as nanocarriers to smuggle antimicrobial compounds. An octaarginine conjugate of an imidazoacridinone derivative (Compound 1-R8) synthetized by us exhibited high antifungal activity against reference...
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Optimization of carbamazepine photodegradation on defective TiO2-based magnetic photocatalyst
PublikacjaIn this work, carbamazepine (CBZ) degradation over defective Fe3O4@SiO2/d-TiO2/Pt photocatalyst was studied. Within the titania structure, Ti vacancies and Pt nanoparticles were introduced to enhance the photocatalyst’s light absorption and influence charge carriers’ mobility. For the carbamazepine degradation, process parameters, e.g., temperature, flux intensity, photocatalyst loading, aeration, pH, and addition of H2O2, were optimized...
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Diminshed toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
PublikacjaThe narrow "therapeutic window" of anti-tumour therapy may be the result of drug metabolism leading to the activation or detoxification of antitumour agents. The aim of this work is to examine (i) whether the diminished toxicity of a potent antitumour drug, C-1748, 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine, compared with its 4-demethyl analogue, C-857, results from the differences between the metabolic pathways for the...
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Chemiluminogenic acridinium salts: A comparison study. Detection of intermediate entities appearing upon light generation
PublikacjaThe nine derivatives of acridine-9-carboxylic acid (CMADs) capable for chemiluminescence (CL), representing various classes of compounds were isolated in a chemically pure state (assessed by RP-HPLC) and identified using high resolution mass spectrometry (ESI-QTOF) and magnetic resonance (1H NMR) techniques. Among them are aryl acridinium esters, containing certainly selected and located substituents in both aromatic systems, an...