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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Synthesis Of A Sulfur Variant For Treatment Of Trypanosomiasis, Carlos Vera-Esquivel Mar 2019

Synthesis Of A Sulfur Variant For Treatment Of Trypanosomiasis, Carlos Vera-Esquivel

Student Research and Creative Activity Fair

Previous work in our lab has found diphenyl ether benzylamines showed a successful response with a micromolar concentration of our lead compound to treat the deadly Trypanosamiosis rhodesience. Furthermore, mammalian cell lines saw promising resistance towards damages. The goal of this study was to synthesize a diphenyl thio benzylamine variant. This variant was more active toward T. b. rhodesience but showed more toxicity to both rat 10 (IC50 mM) and human cell lines (HFF, HC-04, U-2 OS, and HEK293). The selectivity index (ratio of toxicity to activity in the same concentration units (SI)) varied from 55 ...


Docking Studies Of Isoform-Selectivity Of Phosphatidylinositol 3-Kinase (Pi3k) Inhibitors, Kaitlin Goettsch Mar 2017

Docking Studies Of Isoform-Selectivity Of Phosphatidylinositol 3-Kinase (Pi3k) Inhibitors, Kaitlin Goettsch

Student Research and Creative Activity Fair

Phosphatidylinositol 3-kinases (PI3Ks) and their related pathways are reputed targets for drug-based anticancer therapies. Mutations in PI3K genes, expression, and pathways are frequent among multiple cancer types. Four isoforms of PI3Ks exist: α, β, γ, & δ and studies have identified several ligands for each isoform which are capable of serving as inhibitory therapeutic compounds. However, the biochemical efficacy of these molecules varies and the isoform selectivity is not well understood. In this study, we applied in silico docking methods and free energy calculation methods to estimate the binding of reported PI3K ligands against 5 PI3K structures: PI3Kα (PBD ID: 2RD0 ...


Comparison Of Conventional And Microwave-Assisted Synthesis Of Chemokine Receptor Type 4 (Cxcr4) Antagonists, Saniya Virani, Damilola Gbadebo, Theresa D. Gaines, Francisco Javier Garcia Apr 2016

Comparison Of Conventional And Microwave-Assisted Synthesis Of Chemokine Receptor Type 4 (Cxcr4) Antagonists, Saniya Virani, Damilola Gbadebo, Theresa D. Gaines, Francisco Javier Garcia

Georgia State Undergraduate Research Conference

No abstract provided.


Synthesis Of Bis-Styrylbenzene Derivatives Via Wittig-Horner Reaction, Joseph K. Wray, Tae Soo Jo, Pradip K. Browmik Aug 2010

Synthesis Of Bis-Styrylbenzene Derivatives Via Wittig-Horner Reaction, Joseph K. Wray, Tae Soo Jo, Pradip K. Browmik

Undergraduate Research Opportunities Program (UROP)

Alzheimer’s Disease is now one of the most common diseases affecting the elderly population. Recently, bis-styrylbenzene derivatives have been shown to reduce the formation of Beta-amyloid plaques in the brain which are profoundly correlated with this disease. Finding new biologically active compounds which can reduce or prevent Alzheimer’s Disease has drawn much attention over the past few decades. Georg Wittig, Nobel Prize Winner in Chemistry, 1979.