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A review of the literature on the biological activity of bis-acridines (diacridines) and tetrakis-acridines (tetra-acridines) is presented. Chemical structures of the most active derivatives are provided. In particular, the last d...
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A review of the literature on the biological activity of bis-acridines (diacridines) and tetrakis-acridines (tetra-acridines) is presented. Chemical structures of the most active derivatives are provided. In particular, the last decade's literature on the subject is discussed. (C) 2017 Elsevier B.V. All rights reserved.
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The title compound, C15H11NO3, belongs to a series of new potential antiviral agents against the herpes virus containing a fused ring system. The acridinone skeleton adopts a boat conformation, with greater folding at the junction...
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The title compound, C15H11NO3, belongs to a series of new potential antiviral agents against the herpes virus containing a fused ring system. The acridinone skeleton adopts a boat conformation, with greater folding at the junction with the dioxane ring. This ring is twisted with an approximate twofold axis bisecting the two C-C bonds. [References: 10]
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During the last years, the discovery of new anticancer drugs remains the mains concerns in oncology, The natural environment has always been a very important source of active Biological molecules and which 60% of the cancer drugs ...
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During the last years, the discovery of new anticancer drugs remains the mains concerns in oncology, The natural environment has always been a very important source of active Biological molecules and which 60% of the cancer drugs used currently are original from a natural products. H.albus is a plant which belongs to Solanaceae family, used generally in traditional medicine as a nervous sedative and para sympatholytic which is rich source of flavonoid, alkaloids and tropane. The present work is for anobjective to test the methanolic fractions extracted from the Aerial Parts of Hyoscyamus albus collected among aures region in Algeria, and evaluate their cytotoxic activity on different cancercells lines and the characterization of the microscopical morphology of apoptosis cell. The effects of four different selected methanolic fractions of H.albusextract( D, E, F, G)obtained by column chromatography over Sephadex LH-20 tested on DU-145, PC-3, U-87 MG and U-373 MG cancer cells lines were determined using MTT [3-(4,5-dimethylthiazolyl)-2,5-diphenyl-tetrazolium bromide] assay and the cell were marked by orange acridine to visualize the apoptotic cells. Our results indicated that the fraction C has a cytotoxic activity against cells lines showed a marked anti-cancer activity with IC50 = 73 mug/ml, 187 mug/ml, 96 mug/ml and 114 mug/ml for the DU-145, PC-3, U-87 MG and U-373 MG respectively, the morphotype apoptotic cell have showed the morphological change which attempt an apoptotic cell marked by a fluorescence. Therefore, the fraction D had just an activity against DU-145 with IC50=186 mug/ml, the fraction F has an IC50 =165 mug/ml and 198 mug/ml against DU-145 and PC-3 respectively. The fraction G showed the activity against DU-145, LNCaP and U-373 MG. The results demonstrated the anticancer properties of H.albusand reveal the therapeutic potential of this plant.
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It was found that the quantum yield of 9-azidoacridine photodissociation was equal to 0.95 ( in acetonitrile) and remained unchanged upon protonation. Quantum-chemical calculations on the structures of the azide and its cation in ...
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It was found that the quantum yield of 9-azidoacridine photodissociation was equal to 0.95 ( in acetonitrile) and remained unchanged upon protonation. Quantum-chemical calculations on the structures of the azide and its cation in the ground (S-0) and the lower singlet excited (S-1) state were performed using semiempirical (PM3) and ab initio (HF, B3LYP) methods. The sigma(*)(NN) antibonding orbital at the N-N-2 bond was occupied in both of the azides in the S-1 state; this fact is consistent with the photochemical activity of these compounds. Because of the presence of absorption bands in the visible region of the spectrum, 9-azidoacridinium hydrochloride is sensitive to visible light, and, among all of the currently known arylazides, it is sensitive to light with the longest wavelength: the quantum yield of its photodissociation is 0.65 on irradiation with 470-nm light.
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Acridine and acridine derivatives have been converted directly to phenyl derivatives regioselectivity using phenyllithium.Alkylation of acridine and acridine derivatives improves their solubility in common organic solvents.
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Newly synthesized 4,5-di-substituted acridines were assessed for in vitro antileishmanial activities as compared to those of their 4-mono-substituted homologues. Mono-substituted acridines exhibited a weak specificity for Leishman...
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Newly synthesized 4,5-di-substituted acridines were assessed for in vitro antileishmanial activities as compared to those of their 4-mono-substituted homologues. Mono-substituted acridines exhibited a weak specificity for Leishmania parasites. Di-substi-tuted acridines, on the contrary, displayed interesting amastigote-specific activities through a mechanism of action that might not involve intercalation to DNA. This antileishmanial property, associated with a low antiproliferative activity towards human cells, led to the identification of a new class of promising acridine derivatives such as 4,5-bis(hydroxymethyl)acridine with a nonclassical mechanism of action based on the inhibition of Leishmania internalization within macrophages. In the meantime, the effects of experimental lighting on the biological properties of acridines were assessed: experimental lighting did not significantly improve the antileishmanial activity of the compounds since it produced a greater toxicity against human cells.
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In near neutral to weak basic media, sodium carboxymethyl cellulose (NaCMC) will dissociate to become a macro polymeric anion, which can react with acridine yellow (AY) or acridine orange (AO) to form an ion-association complex re...
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In near neutral to weak basic media, sodium carboxymethyl cellulose (NaCMC) will dissociate to become a macro polymeric anion, which can react with acridine yellow (AY) or acridine orange (AO) to form an ion-association complex resulting in fluorescence quenching of the acridine dyes. The maximum fluorescence quenching wavelength is 505 nm (lambda(ex) = 440 nm) for AY system and 530 nm (lambda(ex) = 493 nm) for AO system, respectively. The fluorescence quenching values (Delta F) are directly proportional to the concentrations of NaCMC and the linear ranges are 20.0-4000 mu g/L for AY system and 20.0-7000 mu g/L for AO system, separately. This method has high sensitivity and the detection limits for NaCMC are 58.0 mu g/L (AY system) and 157.2 mu g/L (AO system). The effects of coexistent substance have been investigated, and the results show that this method has a relatively good selectivity. A fluorescence quenching method for the determination of NaCMC based on the ion-association reactions of CMC polymeric anion with a basic acridine dye was developed. The method is sensitive, simple and fast. (c) 2005 Elsevier B.V. All rights reserved.
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Oxadisilole-fused acridines, dioxatrisilole-fused acridines and benzo[b]acridines were synthesized through nucleophilic additions and aromatization reactions of arynes with 2-aminoaryl ketones or 2- aminoaryl aldehydes in good yie...
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Oxadisilole-fused acridines, dioxatrisilole-fused acridines and benzo[b]acridines were synthesized through nucleophilic additions and aromatization reactions of arynes with 2-aminoaryl ketones or 2- aminoaryl aldehydes in good yields at room temperature. The photophysical, redox and thermal properties of these compounds were characterized. These compounds show potential applications as strong deep-blue or green emitters for OLED because of high fluorescence quantum yields and good thermal stabilities.
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Acridinium salts 3a-h were synthesized from the corresponding sulfonamides 1a-h and their chemiluminescence profiles were compared. The quantity of light emitted over the time studied did not correlate well with the pK_a of sulfon...
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Acridinium salts 3a-h were synthesized from the corresponding sulfonamides 1a-h and their chemiluminescence profiles were compared. The quantity of light emitted over the time studied did not correlate well with the pK_a of sulfonamide leaving group. Rather, steric factors contributed the most to modulating the light output from these compounds. The mesitylsulfonyl substituent of acridinium salt 3d reduced the chemiluminescence signal by 20-fold relative to the reference acridinium salt 3a.
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Steady-state and time-resolved fluorescence and UV-vis techniques were used to study the formation and dissociation of acridine orange dimer in order to investigate hyaluronan-acridine orange, hyaluronan-CTAB (cetyltrimethylammoni...
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Steady-state and time-resolved fluorescence and UV-vis techniques were used to study the formation and dissociation of acridine orange dimer in order to investigate hyaluronan-acridine orange, hyaluronan-CTAB (cetyltrimethylammonium bromide), polystyrenesulfonate-acridine orange, and polystyrenesulfonate-CTAB interactions in aqueous solution. Steady-state and time-resolved fluorescence and the dimer:monomer absorbance ratio of acridine orange (AO) were used to determine dimer formation on polymer chains of polyelectrolytes. Acridine orange clearly formed dimers on polystyrensulfonate chains as well as on hyaluronan, but we show that the electrostatic interaction is much weaker in the case of hyaluronan. After the addition of surfactant, we observed an enhancement of fluorescence intensity, indicating the dissociation of AO dimers into monomers and the replacement of acridine orange on polymer chains by surfactant molecules. Importantly, we show that surfactant molecules bind to polymer chains before the critical micelle concentration is reached and form the so-called "bottle-brush" structure.
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