groove binders
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 of the ...
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Turning intercalators into groove binders: synthesis, photophysics and DNA binding properties of tetracationic mononuclear ruthenium(ii)-based chromophore-quencher complexes.
... 1 more author 2018 Turning intercalators into groove binders: synthesis, photophysics and DNA binding properties of tetracationic mononuclear rutheniumii-based chromophore-quencher compl[r] ...
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Four pyrrole derivatives used as building blocks in the synthesis of minor groove binders
... 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 ...minor ...
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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 ...minor groove binder. In the case of other classes of minor ...
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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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Design, synthesis and antibacterial activity of minor groove binders: the role of non-cationic tail groups
... minor groove binder rather than any intrinsic property of the ...minor groove binders with both nitroalkenyl (11a,c) and tri- fl uoroacetamido (14c) tail groups showed signi fi cant antibacterial ...
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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 a good ...
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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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Turning intercalators into groove binders: synthesis, photophysics and DNA binding properties of tetracationic mononuclear ruthenium(ii)-based chromophore-quencher complexes.
... optical spectroscopy and computational studies confirm that the bipyridyldiylium moiety has a low-lying reduction that quenches the 3 MLCT-based emission usually observed in such systems. The new complexes interact with ...
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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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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
... The authors [14] designed their compounds on the basis of the tail region, which is the portion of the molecule that contains cationic groups Figure 3. It is known that the positive charge of the tail should interact ...
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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
... minor groove binders against other infectious organisms, particularly parasites, was also being ...minor groove binders did not show toxicity to the animals at therapeutically effective doses ...
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Entropic binding mode preference in cooperative homo-dimeric drug-DNA recognition
... 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 binding of two ...
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Racial Disparity in Social Spatiality: Usage of National Parks and Opera Attendance
... AT-minor groove binders using biosensor-SPR technique show that the inhibitory ranking order is consistent with that of binding affinity and linear-shaped DB921 still has excellent inhibitory ...minor ...
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Constructing Empirical Likelihood Confidence Intervals for Medical Cost Data with Censored Observations
... minor groove binding compounds, have been shown to inhibit interactions of transcription factors binding to genomic ...minor groove binders typically recognize DNA at A-tract or alternating A·T base ...
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A review study on asphalt binders
... The substance of desulfurized rubber powder clearly affected the blending effort and execution of resultant DRA covers. To get a suitable substance, cover tests were led on DRA binders with various substance (i.e., ...
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Tomographic docking suggests the mechanism of auxin receptor TIR1 selectivity
... potential binders (electronic supplementary material, figure S2), namely indole-3-carboxylic acid (ICA), indole-3-propio- nic acid (IPA), indole-3-butyric acid (IBA), indol-3-yl acetate (IDA), 1-naphthaleneacetic ...
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