- Modular preparation of diverse dipyrrolemethanes
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A modular synthesis of polyfunctional dipyrrolemethanes is presented. Diverse side chains are introduced to 2-carboxypyrrole building blocks in two to four steps, resulting in a collection of substituted pyrroles that, when condensed in one step, give ris
- Pham, Cindy C.,Park, Michelle H.,Pham, Jenny Y.,Martin, Sadie G.,Schramm, Michael P.
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p. 1165 - 1173
(2013/06/05)
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- A sweet origin for the key congocidine precursor 4-acetamidopyrrole-2- carboxylate
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Feeding (Streptomyces) frenzy: Natural products belonging to the pyrrolamide family are defined by their pyrrole-2-carboxamide moiety. 4-acetamidopyrrole-2-carboxylate is identified as the key pyrrolamide congocidine precursor (see scheme) through feeding studies using Streptomyces ambofaciens. The biosynthetic pathway of congocidine starts with the carbohydrate N-acetylglucosamine and involves carbohydrate-processing enzymes. Copyright
- Lautru, Sylvie,Song, Lijiang,Demange, Luc,Lombès, Thomas,Galons, Hervé,Challis, Gregory L.,Pernodet, Jean-Luc
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supporting information; experimental part
p. 7454 - 7458
(2012/09/21)
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- 2,3-SUBSTITUTED AZAINDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS
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The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3-Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted Azaindole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
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Page/Page column 77-78
(2009/04/25)
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- PYRROLO [3, 2-A] PYRIDINE DERIVATIVES FOR INHIBITING KSP KINESIN ACTIVITY
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The present invention provides compounds of Formula I (wherein R, R1, R3, R4, X, and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
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Page/Page column 73
(2008/12/07)
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- Recognition of the DNA minor groove by pyrrole-imidazole polyamides: Comparison of desmethyl- and N-methylpyrrole
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Polyamides consisting of N-methylpyrrole (Py), N-methylimidazole (Im), and N-methyl-3-hydroxypyrrole (Hp) are synthetic ligands that recognize predetermined DNA sequences with affinities and specificities comparable to many DNA-binding proteins. As derivatives of the natural products distamycin and netropsin, Py/Im/Hp polyamides have retained the N-methyl substituent, although structural studies of polyamide:DNA complexes have not revealed an obvious function for the N-methyl. In order to assess the role of the N-methyl moiety in polyamide:DNA recognition, a new monomer, desmethylpyrrole (Ds), where the N-methyl moiety has been replaced with hydrogen, was incorporated into an eight-ring hairpin polyamide by solid-phase synthesis. MPE footprinting, affinity cleavage, and quantitative DNase I footprinting revealed that replacement of each Py residue with Ds resulted in identical binding site size and orientation and similar binding affinity for the six-base-pair (bp) target DNA sequence. Remarkably, the Ds-containing polyamide exhibited an 8-fold loss in specificity for the match site versus a mismatched DNA site, relative to the all-Py parent. Polyamides with Ds exhibit increased water solubility, which may alter the cell membrane permeability properties of the polyamide. The addition of Ds to the repertoire of available monomers may prove useful as polyamides are applied to gene regulation in vivo. However, the benefits of Ds incorporation must be balanced with a potential loss in specificity. Copyright (C) 2000 Elsevier Science Ltd.
- Bremer, Ryan E.,Szewczyk, Jason W.,Baird, Eldon E.,Dervan, Peter B.
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p. 1947 - 1955
(2007/10/03)
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