MINOR-GROOVE BINDERS
Four pyrrole derivatives used as building blocks in the synthesis of minor groove binders
... of minor-groove binders (MGBs) has expanded vastly and now these compounds display a wide spectrum of biological activities, such as anti- bacterial, antifungal, antiparasitic and anticancer ...the ...
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Design, synthesis and antibacterial activity of minor groove binders: the role of non-cationic tail groups
... non-cationic minor groove binders with neutral tail groups attached to the three backbones that gave highest antibacterial activity in earlier studies ...
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Minor groove binders for DNA as antitypanosomal agents : the veterinary context
... The metabolomics observations can be compared with the results from RNA-seq experiments using another S-MGB (3) attacking Staphylococcus aureus (see paper ‘Why antibacterial minor groove binders are ...
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Four pyrrole derivatives used as building blocks in the synthesis of minor-groove binders
... amido)-N-[2-(morpholin-4-yl)ethyl]-1H-pyrrole-2-carboxamide}, are inter- mediates used in the synthesis of modified DNA minor-groove binders. In all four compounds, the nitro groups lie in the plane ...
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Why antibacterial minor groove binders are a good thing
... processes associated with cell wall integrity and energy production are affected. Attempts to generate resistant strains have failed. Taken together, these properties identify Strathclyde minor groove ...
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An evaluation of minor groove binders as anti-lung cancer therapeutics
... Minor groove binders that have seen use previously as anti-cancer agents are often modified with an DNA-alkylating moiety, such as in ...of minor groove binder. In the case of other ...
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An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics
... General synthesis of head group for amidine linked MGB The appropriate thioamide 0.55 mmol was suspended in acetone 25 mL, dry to which iodomethane 200 mL was added and the reaction mixt[r] ...
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An evaluation of minor groove binders as anti-fungal and anti-mycobacterial therapeutics
... The reaction mixture was left standing at room temperature overnight and then the solvent was removed and the residue was dissolved in DMF 1 mL.. HPLC purification Rt = 22 min followed b[r] ...
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Evaluation of minor groove binders (MGBs) as novel anti-mycobacterial agents, and the effect of using non-ionic surfactant vesicles as a delivery system to improve their efficacy
... delamanid, bedaquiline and pretomanid, and only ten new 67 drugs are in advanced phases of clinical trials as of 2016.7, 8 With the slow development of 68 major advances in anti-mycobact[r] ...
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Minor groove binders: some recent research in drug development
... geometry best suited to fitting in the groove. However, Boykin et al. have shown that linear molecules are also capable of strongly binding to the minor-groove [12]. Therefore the curvature is not ...
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DNA minor groove binders-inspired by nature
... Two molecules of this compound bind side-by-side in the minor groove however, MGBs containing one or more heterocyclic rings other than pyrrole 100 because of the bulky “isopropyl” of th[r] ...
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Selectivity in anti-infective minor groove binders
... Summary of SAR Across Organisms Structural Feature Effect on Organism Selectivity Large head group No apparent selectivity, but all active compounds have a larger head group than distamy[r] ...
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The antibacterial drug MGB-BP3 : from discovery to clinical trial
... Strathclyde minor groove binders against other infectious organisms, particularly parasites, was also being ...effective minor groove binders did not show toxicity to the animals ...
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Thiazotropsin aggregation and its relationship to molecular recognition in the DNA minor groove
... Nuclear Magnetic Resonance (NMR) spectroscopy and isothermal titration calorimetry (ITC) studies of DNA binding by the thiazotropsin class of molecules show no observable evidence of single molecule binding in a ...
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Ranking ligand affinity for the DNA minor groove by experiment and simulation
... Abstract: The structural and thermodynamic basis for the strength and selectivity of the interactions of minor-groove binders (MGBs) with DNA is not fully understood. In 2003 we reported the first ...
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Entropic binding mode preference in cooperative homo-dimeric drug-DNA recognition
... DNA minor groove binders (MGBs), involving the formation of a dimer in free solution followed by the binding of that dimer to DNA, which contrasts with the sequential or simultaneous cooperative ...
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Sequence-selective minor groove recognition of a DNA duplex containing synthetic genetic components
... impact minor groove ...other minor groove binders such as Hoechst33258 in complex with A-tract dsDNA ...uences groove width but also reduces allosteric modulation in a DNA ...of ...
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Comparative effects of A.T and G.C sequence selective DNA minor groove binding agents
... involving minor groove binders and DNA processing enzymes demonstrate inhibition of the proteins, there are some reports of an increase in enzyme activity in the presence of minor ...
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Superresolution imaging of single DNA molecules using stochastic photoblinking of minor groove and intercalating dyes
... and minor groove binders, which attach between the helical ...the minor groove binders, such as SYTO-13, have been less well studied despite being potentially less perturbative ...
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Constructing Empirical Likelihood Confidence Intervals for Medical Cost Data with Censored Observations
... of minor groove binding compounds, have been shown to inhibit interactions of transcription factors binding to genomic ...polyamides, minor groove binders typically recognize DNA at ...
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