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Berlin Brandenburg

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  • 1
    Language: English
    In: Tetrahedron Letters, 15 May 2013, Vol.54(20), pp.2525-2527
    Description: Adenine was formed when an aqueous solution of CH COONH /NH HCO was subjected to mass spectrometer/refluxed for 72 h/heated in a closed vessel for a long time. Since these salts are sources of CO and NH and H O is available from the reaction medium, adenine might get formed by the combination of CO , H O and NH . The occurrence of this reaction in the gas phase as well as in the aqueous phase points towards the possibility of similar reactions during the primitive earth conditions.
    Keywords: Adenine ; Gas Phase Reactions ; Mass Spectrometer ; Solution Phase Reaction ; Chemistry
    ISSN: 0040-4039
    E-ISSN: 1873-3581
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  • 2
    Language: English
    In: Bioorganic & Medicinal Chemistry Letters, 01 March 2013, Vol.23(5), pp.1433-1437
    Description: A series of highly promising 5-LOX inhibitors was identified. Based upon the structures of some known 5-LOX inhibitors, a set of five compounds carrying appropriate substituents at N-1 and C-3 of indole were synthesized and investigated for 5-LOX inhibitory activities. Fifty percent inhibitory concn (IC ) of these compounds ranges from 0.6 to 5 μM and found to be comparable to that of clinically used 5-LOX inhibitor, zileuton. The compounds under present investigations exhibited appreciable interactions with 5-LOX as apparent from their association constants calculated from the mass spectral data. Compound with a tosyl group at N-1 and pyrolidinyl-1,2-dione substituent at C-3 of indole, exhibiting IC 0.6 μM and stoichiometry of 1:7 in the enzyme–compound complex was identified as highly potent 5-LOX inhibitor and seems to be suitable for further investigations.
    Keywords: 5-Lipoxygenase ; Indole Derivatives ; Inhibitors ; Mass Spectra ; Docking ; Medicine ; Chemistry ; Anatomy & Physiology
    ISSN: 0960-894X
    E-ISSN: 1464-3405
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  • 3
    Language: English
    In: Bioorganic & Medicinal Chemistry Letters, 15 September 2015, Vol.25(18), pp.3854-3858
    Description: In order to develop the amino acid appended acridines as potential leads for anticancer drugs, they were subjected to preliminary investigations. Screening through MTT assay as well as the phase contrast micrographs and Confocal images of immunostained C6 Glioma cells for markers such as α-tubulin, GFAP, mortalin and HSP-70 cells indicated that the compounds possess significant antiproliferative activity. The compounds also arrested cells in G /G phase of the cell cycle as indicated by flow cytometry results. Moreover, the upregulation of the senescence markers such as mortalin and HSP70 in the presence of compounds , and indicate their senescence inducing potential.
    Keywords: Acridines ; Antiproliferative ; C6 Glioma Cells ; Α-Tubulin, Gfap, Mortalin and Hsp-70 Markers ; Medicine ; Chemistry ; Anatomy & Physiology
    ISSN: 0960-894X
    E-ISSN: 1464-3405
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  • 4
    Language: English
    In: Bioorganic & Medicinal Chemistry Letters, 01 January 2014, Vol.24(1), pp.77-82
    Description: Six molecules were obtained by the combination of three biologically and medicinally significant moieties—indole, chrysin and pyrazole. Bio-evaluation of these hybrid molecules showed significant inhibition of COX-2 enzymatic activity over that of COX-1 and appreciable anti-nociceptive activity, checked at swiss albino mice.
    Keywords: Chrysin ; Indole ; Anti-Inflammatory ; Anti-Nociceptive ; Molecular Modeling ; Medicine ; Chemistry ; Anatomy & Physiology
    ISSN: 0960-894X
    E-ISSN: 1464-3405
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  • 5
    In: Chemical Communications, 2011, Vol.47(15), pp.4472-4474
    Description: Acridones carrying an appropriate substituent at N-10 showed significant fluorescence changes on interacting with ATP in HEPES buffer at pH 7.2. The selectivity and sufficient binding of these probes with ATP could be useful for monitoring of metabolic processes.
    Keywords: Acridines -- Chemistry ; Adenosine Triphosphate -- Chemistry ; Fluorescent Dyes -- Chemistry;
    ISSN: 1359-7345
    E-ISSN: 1364-548X
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  • 6
    In: Chemical Communications, 2011, Vol.47(32), pp.9122-9124
    Description: Compound 4 removes cyanide from water and human serum in the form of compound 7 (cyano-derivative of 4 ) and experiments show its suitability as an antidote of CN poisoning.
    Keywords: Antidotes -- Chemistry ; Cyanides -- Isolation & Purification ; Serum -- Chemistry;
    ISSN: 1359-7345
    E-ISSN: 1364-548X
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  • 7
    Language: English
    In: Tetrahedron Letters, 09 April 2014, Vol.55(15), pp.2467-2470
    Description: A highly convenient method for breakdown of cellulosic material to its monomeric units is devised. Microwave irradiation of aqueous solution of cellulose in the presence of NaF/NaCl resulted into disintegration of cellulose to its monomeric unit, glucose (55%) in 20 min.
    Keywords: Cellulose ; Microwaves ; Hydrolysis ; Glucose ; Chemistry
    ISSN: 0040-4039
    E-ISSN: 1873-3581
    Source: ScienceDirect Journals (Elsevier)
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  • 8
    Language: English
    In: Journal of medicinal chemistry, 26 July 2012, Vol.55(14), pp.6381-90
    Description: On the basis of structural analysis of dihydrofolate reductase (DHFR) (cocrystallized separately with NADPH, dihydrofolate and NADPH, trimethoprim), compounds 2 and 3 were optimized for inhibition of DHFR. Appreciable tumor growth inhibitory activities of compounds 2 and 3 over 60 human tumor cell lines were recorded. Combination of syringaldehyde and indole moieties in these two compounds was rationalized by the synthesis of compounds 4-7, 10, and 11, which were found to have less tumor growth inhibitory activities than compounds 2 and 3. Further, UV-vis and NMR spectral investigations showed significant interactions of compounds 2 and 3 with DHFR and inhibition of its catalytic activity was observed in the presence of these compounds. Therefore, modification of trimethoprim, an antibacterial drug with no tumor growth inhibition, led to the development of compounds 2 and 3 having appreciable anticancer activities that seem to be due to inhibition of DHFR.
    Keywords: Drug Design ; Antineoplastic Agents -- Chemistry ; Folic Acid Antagonists -- Chemistry ; Tetrahydrofolate Dehydrogenase -- Metabolism
    ISSN: 00222623
    E-ISSN: 1520-4804
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  • 9
    Language: English
    In: Journal of Medicinal Chemistry, 02/14/2013, Vol.56(3), pp.1361-1361
    ISSN: 0022-2623
    E-ISSN: 1520-4804
    Source: American Chemical Society (via CrossRef)
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  • 10
    Language: English
    In: Bioorganic & Medicinal Chemistry, 01 March 2014, Vol.22(5), pp.1642-1648
    Description: N-1 tosyl indoles carrying amino acid as a part of C-3 substituent are identified with considerable 5-LOX inhibitory activities. On the basis of enzyme inhibitory activities and log , it is found that these compounds are more suitable to use as ester prodrugs. In addition to the significant and for 5-LOX, advantageously the compounds under present investigation do not affect the viability of the cell. The experimental results were also supported by molecular docking of compounds in the active site of 5-LOX.
    Keywords: Indole ; Amino Acid ; 5-Lox Inhibition ; Molecular Modeling ; Medicine ; Chemistry ; Anatomy & Physiology
    ISSN: 0968-0896
    E-ISSN: 1464-3391
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