Novel Silylated Small Molecule Derivatives as Anticancer Agents (2021-04-02)

Abstract

Applications of silicon based protecting groups appear to not be limited tochemical synthesis, but also have practical drug applications. Implementationof novel silicon-based derivatives on pharmaceutically active templates is asimple tactic to decrease harmful side effects, increase drug permeability, whilealso providing a capable prodrug that’s selective toward acidic environments.Metabolic enzymatic reactions convert therapeutics into polar metabolites thatare easily removed from the body, however enzymatic reactions require specificligand configurations. Silicon represents a foreign element that does not fit themetabolic configuration to be broken down. This slows metabolic processesincreasing drug latency, maintaining therapeutic benefits, and eliminating toxicside effects from secondary metabolites. Silicon derivatives also show benefitby increasing lipophilicity compared to carbon. This increase in lipophilicity hasled to many therapeutic benefits like improved cell penetration and increaseddrug permeability across the blood-brain barrier. In addition, silyl etherderivatives also have a suitable use as prodrugs of pharmaceutically activecompounds, this would increase the drug latency and improve the drugselectivity to acidic environments commonly associated with cancerous tissues.With the added benefits of silicon derivatives on pharmaceutically activetemplates, it is hypothesized that silicon protecting will enhance the cytotoxicityand lipophilicity of the candidate compounds. Further investigation on themedicinal advantages of silicon derivatives on drug derivatives will bedemonstrated using quinoline templates. Synthesized silicon drug candidateswere tested on different cancer cells using MTT cell viability assay to evaluatethe cytotoxic properties. In this seminar, I will present my synthetic and in vitrobiological results.