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Physical Sciences and Mathematics Commons

Open Access. Powered by Scholars. Published by Universities.®

Conference

University of Nebraska at Omaha

Chemistry

2017

Articles 1 - 4 of 4

Full-Text Articles in Physical Sciences and Mathematics

Synthesis Of Small Molecule Anti-Trypanosomal Drugs, Samuel Anderson Mar 2017

Synthesis Of Small Molecule Anti-Trypanosomal Drugs, Samuel Anderson

UNO Student Research and Creative Activity Fair

Demand for novel chemotherapeutic agents that treat Human African Trypanosomaiasis (HAT) persists. A series of compounds sharing a 3,4’diphephyl ether skeleton were prepared for a structure activity relationship (SAR) study evaluating antitrypansomal drug candidates. Trypanocidal assays performed in vitro by the Swiss Tropical and Public Health Institute identified a lead with an IC50 of 1.35 μg/mL analogous to a compound previously made in our laboratory. A slight improvement in activity (10%) was observed when changing the molecular substitution pattern from 4,4’ to 3,3’; however, the result is equivocal. Furthermore, in vitro test results demonstrated the weakness of amides as side …


Could O-Aminoquinones Of Estrogen Metabolites Serve As Platforms For Redox Cycling?, Rachel Miller Mar 2017

Could O-Aminoquinones Of Estrogen Metabolites Serve As Platforms For Redox Cycling?, Rachel Miller

UNO Student Research and Creative Activity Fair

The metabolism of estrogen can lead to the formation of two isomeric o-quinones, estrogen-2,3-quinone (E-2,3-Q) and estrogen-3,4-Q (E-3,4-Q). The more reactive E-3,4-Q is genotoxic and can damage DNA by forming apurinic sites; whereas, E-2,3-Q does not form apurinic sites. Estrogen quinones may also be involved in redox cycling to produce reactive oxygen species (ROS), which is another genotoxic pathway. What is not yet clear, is why E-3,4-Q would undergo redox cycling while the non-carcinogenic E-2,3-Q would not. Nitrogen nucleophiles react with the E-3,4-Q at the 1-position. With DNA bases as the nitrogen (sp2) nucleophile, the adducts formed are catechols. We …


Characterization Of The Mannose-6-Phosphate/Insulin-Like Growth Factor Ii Receptor Using 1-3mh, Zechariah Craig Mar 2017

Characterization Of The Mannose-6-Phosphate/Insulin-Like Growth Factor Ii Receptor Using 1-3mh, Zechariah Craig

UNO Student Research and Creative Activity Fair

The mannose-6-phosphate/insulin-like growth factor 2 receptor (M6P/IGF2R), a recombinant triplet protein receptor for studies involving receptor dimerization, plays a pivotal role in mediating cellular growth. This receptor is comprised of fifteen similar units that fold into five triplet subunits. The goal of this experiment is to investigate how to make the 1-3MH protein more stable at the DNA level and generate a larger yield from DNA extractions for more effective transfections. This was accomplished by minorly changing the protocols for the DNA purification. Instead of using a standard column DNA purification kit, a crude DNA purification was done instead. This …


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

UNO 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: …