Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 7 of 7 for “"complexity to diversity"”.
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Discovery of covalent modifiers via the complexity to diversity strategy
… have been developed as a promising alternative to discover and validate novel targets. However, most covalent screening libraries consist of flat, low molecular weight compounds that are lacking in complexity and are incapable of addressing more complex targets, such as protein-protein …
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Chemical diversification and anticancer activity of natural products
Made available in DSpace on 2014-01-16T18:25:34Z (GMT). No. of bitstreams: 3 Karen_Morrison.pdf: 14532423 bytes, checksum: af6a40d935f8782447ddd84ef12a94ae (MD5) Morrison_Karen.docx: 44256739 bytes, checksum: 6353cc66b66320dd9c663bda8c68747b (MD5) license.txt: 4063 bytes, checksum: …
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Discovery and biological evaluation of ferroptocide
… for biological discovery. Herein, we subject the complexity-to-diversity library of compounds to an anticancer phenotypic screen. This effort resulted in identification of an active class of compounds derived from pleuromutilin natural product. Biological evaluation identified the novel compound …
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Chemical diversification of the natural products quinine, abietic acid and pleuromutilin by ring distortion
Ring distortion reactions directly alter the core ring systems of small molecules and can lead to striking changes in molecular structure. Strategic application of ring distortion reactions to complex molecules, such as natural products, is an effective method for the generation of compounds that …
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The influence of positively charged nitrogen species on compound accumulation and activity in gram-negative bacteria
… these infections constitute a major threat to human health. A significant challenge is the inability of most compounds to accumulate in Gram-negative bacteria. Recently developed predictive guidelines called the eNTRy rules show that appending a primary amine to an appropriately shaped …
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Ring distortion of the alkaloid sinomenine and novel prodrug approaches to broad-spectrum antibiotics
… bacterial membrane, as it is impermeable to most organic small-molecules. The eNTRy rules, developed by the Hergenrother lab, can guide the synthesis of Gram-negative-active antibiotic leads as they predict the likelihood of compound accumulation in Gram-negative bacteria. In general, for …
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Development of predictive guidelines for compound accumulation in gram-negative bacteria
New antibiotics to combat drug-resistant Gram-negative pathogens are urgently needed. Most small molecules are unable to rapidly traverse the outer membrane of Gram-negative bacteria and accumulate inside these cells, making the discovery of drugs against these pathogens challenging. Current …