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 6 of 6 for “"conformational restriction"”.
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Synthesis of furo[2,3-d]pyrimidines, thieno[2,3- d]pyrimidines, pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolates, receptor tyrosine kinase (RTK) inhibitors and antimitotic agents
… biological evaluation suggest the importance of conformational restriction for activity. Fifty - seven furo[2,3- d ]pyrimidines and six thieno[2,3- d ]pyrimidines were designed on iv the basis of crustal structures and synthesized as potential RTK inhibitors with antimitotic antitumor activity. …
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Synthesis of Biologically Active Tropolones and Stereochemically Rich Compounds via Cross-Coupling Reactions
… is a form of chirality arising from conformational restriction of chiral axes and has an essential role in many compounds including, but not limited to, chiral ligands, and pharmaceutical drugs. Structural aspect of tropolones such as their large ring size, smaller bond angles, …
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Activatable photoacoustic contrast agents for sensing and delivering nitric oxide, and development of small molecule photoacoustic platforms with improved properties for in vivo imaging
… properties of the aza-BODIPY scaffold using conformational restriction (Chapter 4), which represents the first study to investigate the link between structure and ratiometric signal output, followed by my work towards water-soluble congeners that is currently ongoing (Chapter 5). I finish …
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SYNTHESIS, BIOLOGICAL ACTIVITY AND CONFORMATIONAL ANALYSIS OF FRAGMENT ANALOGUES OF ALPHA-MELANOTROPIN (PEPTIDE, STRUCTURE-FUNCTION, PHENYLGLYCINE, NMR, TETRAHYDROISOQUINOLINE-3-CARBOXYLATE).
… enhanced potency. In this regard, a series of conformationally restricted linear and cyclic fragment analogues of α-MSH have been prepared and carefully analyzed by both biological and biophysical methods. Conformational restriction was incorporated in α-MSH fragment analogues, by: (1) …
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Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency
… structural evidence for the presence of a conformationally restricting intramolecular fluorine hydrogen bond have been described. The dissertation also discusses the synthetic efforts for obtaining the pyrrolo[2,3-<em>d</em>]pyrimidine analogs with regioisomeric substitutions, modified …
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Identification and charaeterization of IAPP-derived inhibitors of cytotoxic self-assembly and amyloidogenesis of islet amyloid polypeptide (IAPP) and beta-amyloid peptide (A beta)
… Using a recently developed minimalistic conformational restriction strategy, four double N-methylated IAPP analogues, [(N-Me)G24, (N-Me)I26]-IAPP (IAPP-GI), [(N-Me)A25, (N-Me)L27]-IAPP (IAPP-LA), [(N-Me)F23, (N-Me)A25]-IAPP (IAPP-FA) and [(N-Me)I26, (N-Me)L27]-IAPP (IAPP-LI), have been …