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Search results for: ACRIDONE
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Synthesis and structure-activity studies of peptide-acridine/acridone conjugates
PublicationW artykule opisano strukturę, syntezę i biologiczną aktywność peptydowych koniugatów akrydyny i akrydonu jako potencjalnych leków o aktywności przeciwnowotworowej i przeciwwirusowej.
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Synthesis and Biological Evaluation of Acridine/Acridone Analogs as Potential Anticancer Agents
PublicationAcridine and acridone analogues were prepared by Ullmann condensation and then cyclization reaction. As a result of nucleophilic substitution reaction 1-nitro-9-phenoxyacridine or 1-chloro-4-nitro-9(10H)-acridone with the corresponding peptides, the planned acridine derivatives (10a-c, 12, 17-a-d, 19) have been obtained. The cytotoxic activity of the newly obtained analogs were evaluated against melanotic (Ma) and amelanotic (Ab)...
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Synthesis and antitumor activity of conjugates of muramyldipeptide or normuramyldipeptide with hydroxyacridine/acridone derivatives
PublicationOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej pochodnymi hydroksyakrydyny/akrydonu i dwóch analogów modyfikowanych pochodnymi 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny. Tylko związki zawierające pochodne 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny wykazały wysoką aktywność cytotoksyczną badaną na 60 liniach ludzkich komórek nowotworowych, na nowotwór prostaty i AIDS-related lymphoma (ARL). Związek...
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Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives
PublicationOpracowano warunki reakcji kwasu mykofenolowego z aminowymi pochodnymi akrydyn i akrydonów. Tak otrzymane koniugaty zostały scharakteryzowane, a następnie przebadane in vitro pod względem aktywności przeciwbiałaczkowej oraz immunosupresyjnej.
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Pochodne akrydyny/akrydonu - synteza, aktywność biologiczna i zastosowanie kliniczne = Acridine/acridone derivatives - synthesis, biological activity and clinical application
PublicationAkrydyny/akrydony stanowią grupę związków o bardzo szerokim spektrum aktywności biologicznej, stosowanych jako leki przeciwbakteryjne, przeciwpasożytnicze, przeciwmalaryczne, anty-HIV oraz przeciw-nowotworowe. Obecnie dużym zainteresowaniem cieszą się aminokwasowe i peptydowe analogi akrydyny/akrydonu, które mogą znaleźć zastosowanie w leczeniu chorób opartych na terapii genowej oraz w nowoczesnych metodach diagnostycznych (np....
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublicationMany 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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Natural and synthetic acridines/acridones as antitumor agents: their biological activities and methods of synthesis.
PublicationPraca 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
PublicationImproved 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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Determination of the minimum inhibitory concentration of C-1305 derivatives (IKE1-IKE8) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of acridone derivatives against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 by the modified M27-A3 specified by the CLSI.
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublicationThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...
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Evidence for solid state electrochemical degradation within a small molecule OLED
PublicationAcridone derivative have been synthesised and used as OLED (Organic Light Emitting Diode) emitters which were found to be electroactive. Electrochemical investigations showed a side reaction takes place inside an active layer which diminished the overall device efficiency. By using a dopant and host active layer architecture, the formation of the by product was removed. The by-product was identified as a σ-dimer formed inside an...
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Kamila Rząd dr inż.
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Solid Phase Synthesis and Biological Activity of Tuftsin Conjugates
PublicationNew tuftsin/retro-tuftsin conjugates were designed and synthesized using a classical fluorenylmethoxycarbonyl (Fmoc) solid phase procedure. All the peptide conjugates were divided into three series: 1,4-dihydroxyanthraquinone (type A), 1-nitroacridine (type B), and 4-carboxyacridone (type C) derivatives. In type A conjugates, the N-terminal group of the peptide chain is directly connected to the anthraquinone ring at C1 (Scheme...
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Determination of the minimum inhibitory concentration of C-1311 derivatives (C-1296, C-1410, Compound 1, Compound 1-R8) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of imidazoacridinone derivatives against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 and C. albicans clinical strains by the modified M27-A3 specified by the CLSI.
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Killing kinetics analysis of C-1311 derivative with octaarginine (Compound 1-R8) against Candida albicans
Open Research DataThe datasets contain the results of killing kinetics analysis of imidazoacridinone derivative and fluconazole against C. albicans ATCC 10231. The suspensions of Candida albicans ATCC 10231 cells (500 µL) in RPMI 1640 at cell density of 104 cells /mL were added to 500 µL of RPMI 1640 medium with various concentrations of the compounds, corresponding...
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The absorption and fluorescence spectra of novel bisacridines (IKE15-19, IKE21) and IE10, potential antifungal agents
Open Research DataOptical measurements of novel bisacridines (IKE15-19, IKE21) and IE10 were conducted. The absorption spectra were recorded from 300 to 800 nm. The fluorescence emission spectra were determined with excitation and emission wavelengths described in the file. All measurements were recorded using a multiplate reader, Tecan Spark 10M.
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Determination of the minimum inhibitory concentration of C-1330 derivatives (IKE9-IKE14) against Candida strains
Open Research DataThe datasets contain the results of determining the minimum inhibitory concentration of C-1330 derivatives (IKE9-IKE14) against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 by the modified M27-A3 specified by the CLSI.
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The absorption and fluorescence spectra of C-1305 derivatives (IKE1-IKE8), potential antifungal agents
Open Research DataOptical measurements of C-1305 derivatives (IKE1-IKE8). The absorption spectra were recorded at 300 - 800 nm for solutions with 16 μg / mL derivative concentration. The fluorescence emission spectra were determined at 420-800 nm with the excitation wavelengths 360 or 415 nm for solutions with 1 μg / mL derivative concentration. All measurements were...
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IKE1-IKE3 (C-1305 derivatives) inhibitory effect of the Yeast Topoisomerase II relaxation activity
Open Research DataInhibition of Yeast Topoisomerase II were analyzed according to relaxation assay kit from Inspiralis. Briefly, 250 ng of supercoiled pBR322 DNA, 1 mM ATP, 1-200 μM of analyzed compound were mixed with reaction buffer (1 mM Tris-HCl (pH 7.9), 10 mM KCl, 0.5 mM MgCl 2, 0.2 % (v/v) glycerol). The reaction was initiated by the addition of an enzyme, allowed...