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Novel pyrimidine derivatives to treat Alzheimer’s Disease

Brain penetrating compounds as promising therapeutics for treatment of neurodegenerative disorders. Problem: An estimated 6.2 million Americans live with Alzheimer’s Disease (AD), and this number is projected to reach over 13 million by 2050 with societal costs expected to rise to $1.1 trillion. A key feature of AD-affected brain tissue is the...

Published: 3/16/2021

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Novel inhibitors of ferroptosis

Novel derivatives of oleic acid effectively inhibiting ferroptosis that could be used for treatment of Friedreich Ataxia, neurodegenerative diseases, and neuropsychiatric diseases. Problem: Ferroptosis is a non-apoptotic form of cell death characterized by the iron-dependent accumulation of toxic lipid-reactive oxygen species. Ferroptosis has been...

Published: 10/16/2020

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Reusable silicon-based cross-coupling agents for the production of natural products, pharmaceuticals, and other organic materials

Cross-coupling reactions without the generation of waste productsProblem: Catalytic carbon-carbon bond formation based on cross-coupling reactions (CCRs) plays a central role in the production of natural products, pharmaceuticals, agrochemicals, and organic materials. Coupling reactions with organometallic reagents and organic halides facilitate a plethora...

Published: 3/20/2020

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CD4 mimetic small molecule inhibitors of HIV-1 entry

Therapeutic development for HIV-1 infection and prevention of transmissionProblem: A global pandemic of human immunodeficiency virus (HIV) and acquired immunodeficiency syndrome (AIDS) persists, with about 34 million people worldwide currently infected and 2.5 million people newly infected with the virus annually.Inhibition of the initial HIV entry...

Published: 3/19/2020

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A novel isostere to replace the carboxylic acid functional group in pharmaceuticals and other compounds

Cycloalkyl-dione derivatives with improved pharmacokinetic and toxicological properties for drug designProblem: Isosteric replacement of a specific group of atoms with a moiety with similar physicochemical properties is a strategy employed by medicinal chemists to improve the properties of biologically active compounds. For example, carboxylic acid...

Published: 3/19/2020

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An efficient method to produce high yield analogs of Hemi-Phorboxazole A with anticancer and antifungal activities

A two-step, high yield, method for synthesizing naturally derived, Hemi-Phorboxazole A analogs Problem: (+)-Phorboxazole A and B, extracted from the sponge Phorbas sp., display extraordinary anti-proliferative activity against National Cancer Institute’s (NCI) panel of 60 human tumor cell lines. Due to their complex structures, the reported syntheses...

Published: 3/17/2020

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Phorboxazole compounds as potent anti-tumor agents

Problem: Phorboxazoles are naturally occurring compounds that have been isolated from the marine sponge Phorbas, endemic to the western coast of Australia. Previous screens of phorboxazoles against the National Cancer Institute human cell line panel indicated the most potent cytotoxicity assayed. While the mechanism of action in vivo is unknown, phorboxazole...

Published: 3/5/2020

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