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Generation of libraries of pharmacophoric structures with increased complexity and diversity by employing polymorphic scaffolds.
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Relative inhibition of insect phenoloxidase by cyclic fungal metabolites from insect and plant pathogens.
The fungal metabolite kojic acid, which is produced by Aspergillus and Penicillium species fungi that may be pathogens of both insects and plants, was a significant inhibitor of phenoloxidase of different representative beetle and caterpillar insect species. Fusaric acid and picolinic acid, produced by Fusarium spp., were also significant inhibitors of phenoloxidase, while dipicolinic acid and beauvericin were ineffective at concentrations tested. Previous reports of the ability of kojic and fusaric acid to inhibit defensive enzymes of plants suggest that these compounds may be important in allowing the producing fungi to be pathogens of both insects and plants.
Effect of novel 1-alkyl-3-hydroxy-2-methylpyrid-4-one chelators on uptake and release of iron from macrophages.
The effect of several iron chelators on iron uptake and release by mouse peritoneal macrophages has been investigated. The 1,2-dimethyl (L1) and 1-ethyl-2-methyl (L1NEt) derivatives of 3-hydroxypyrid-4-one markedly enhanced iron mobilisation from macrophages pulsed with 59Fe-transferrin-antitransferrin immune complexes and were more effective than desferrioxamine, maltol, or mimosine. Release increased with increasing chelator concentration. None of the chelators donated significant amounts of iron to macrophages, and none showed any cytotoxic effect. The synthetic alpha-ketohydroxypyridine chelators may therefore be active in removing iron from the reticuloendothelial system as well as from hepatocytes, and indeed may be superior to desferrioxamine.
Total synthesis of (+)-wailupemycin B.
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An efficient and general method for the synthesis of alpha,omega-difunctional reduced polypropionates by Zr-catalyzed asymmetric carboalumination: synthesis of the scyphostatin side chain.
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Total synthesis of (+)-scyphostatin, a potent and specific inhibitor of neutral sphingomyelinase.
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Total synthesis of apoptolidinone.
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Mutasynthesis of aureonitrile: an aureothin derivative with significantly improved cytostatic effect.
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A small-molecule FRET probe to monitor phospholipase A2 activity in cells and organisms.
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Total synthesis of auripyrone A.
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Solution-phase mixture synthesis with fluorous tagging en route: total synthesis of an eight-member stereoisomer library of passifloricins.
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Natural products research: renaissance with strengthened integration of biology and chemistry.
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Enantioselective total synthesis and structure determination of the antiherpetic anthrapyran antibiotic AH-1763 IIa.
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The tubulin-bound conformation of discodermolide derived by NMR studies in solution supports a common pharmacophore model for epothilone and discodermolide.
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Photochemical origin of the immunosuppressive SNF4435C/D and formation of orinocin through "polyene splicing".
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[Pyranylidene-anthrones (author's transl)].
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