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Showing 1 to 5 of 5 for “"Bioisosteric replacements"”.
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Prediction of Metabolic Stability and Bioavailability with Bioisosteric Replacements
… which can carry out SOM predictions, as well as bioisosteric replacement identification. Same as CASSI, this is available via the Coralie application GUI. The bioavailability issues caused by the metabolic enzyme, cytochrome P450 3A4, and transporter protein P-gylcoprotein are also investigated …
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DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL INDENOISOQUINOLINES AS POTENTIAL ANTICANCER AGENTS
… and carbohydrate-mimetic moieties; (3) seek out bioisosteric replacements for the nitro group in the highly active 3-nitroindenoisoquinoline Top1 inhibitor series; and (4) design and test dimeric indenoisoquinolines that could
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Design and Synthesis of Pyrimidine Based Fused Heterocyclics in the Potential Treatment of Cancer and Opportunistic Infection
… the basic principles of scaffold hopping and bioisosteric replacements. The work described herein discusses our efforts to obtain agents with inhibition of two or more intracellular targets to inhibit <em>de novo</em> purine biosynthesis. Synthetic efforts for the development of …
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Target Based Design and Synthesis of Fused Pyrimidines in the Potential Treatment of Cancer and Opportunistic Infection
… the basic principles of scaffold hopping and bioisosteric replacements. The work described herein discusses our efforts to obtain agents with inhibition of two or more intracellular targets to inhibit <em>de novo</em> purine biosynthesis. Synthetic efforts for the development of …
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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
… <p>This dissertation discusses the bioisosteric and regioisomeric optimization of 5-and/or 6-substituted pyrrolo[2,3-<em>d</em>]pyrimidine antifolates for improved tumor-targeted activity. Molecular modeling with the help of known X-ray crystal structures of the transporters and the …