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Download Investigation of drug like scaffolds with anticancer activity
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NUS Graduate School for Integrative Sciences and Engineering Research Project Write-up Title of Project : Investigation of drug like scaffolds with anticancer activity Name of Supervisor : Go Mei Lin Contact Details: [email protected] Tel: 65162654 Short Description Potency is a necessary but not sufficient requirement for target compounds destined for further development along the drug development pipeline. Key target compounds must necessarily be “drug‐like” in order to ensure pharmacokinetic compliance. Drug like features include compliance to solubility and permeability thresholds, non‐aggregating behavior and an acceptable degree of metabolic stability. Our laboratory has been investigating various functionalized scaffolds that have potent antiproliferative activity on cell based assays. However, the drug like profiles of these compounds can be improved and the objective is to find the “structural” sweet spot for potency and druglikeness. The project sequence will broadly involve synthesis, screening for antiproliferative activity, structural refinement of early hits with an eye on drug like features, confirmation of drug like features (solubility, permeability, aggregation, in vitro microsomal metabolism) and mechanistic evaluation. Where applicable, computational approaches will be adopted for compound design and target validation.
