Dr. Sarlah from the University of Illinois has synthesized novel analogs and isotopologs of the anticancer isocarbostyril alkaloids lycoricidine and narciclasine. Currently, isocarbostyril alkaloids are low in natural abundance and have poor aqueous solubility. These new synthetic compounds exhibit improved metabolic activity, stability, and/or aqueous solubility.
Enantioselective Synthesis of Isocarbostyril Alkaloids and Analogs Using Catalytic Dearomative Functionalization of Benzene. Bingham, et al. Dec 6, 2018.
Dr. Paul Hergenrother fhas developed a new series of broad spectrum fusidic acid derivatives. Designed using two distinct methodologies, these fusidic acid derivatives...
Dr. Paul Hergenrother fhas developed a new series of broad spectrum fusidic acid derivatives. Designed using two distinct methodologies, these fusidic acid derivatives feature unique side chains and demonstrate improved MIC values when compared with fusidic acid. One series of derivatives displays antibiotic activity against Gram-negative ESKAPE pathogens, including in clinical isolates of P. aeruginosa. The prodrug displays low toxicity in mammalian cells and human serum experiments suggest that it is less protein bound than Fusidic Acid. A second series of derivatives displays potent activity against clinical isolates of Staphylococcus aureus and Enterococcus faecium and an improved resistance profile in vitro and in vivo when compared to fusidic acid. Additionally, these derivatives display in vivo efficacy against an FA-resistant strain of Staphylococcus aureus in a mouse infection model.
This cancer treatment material and approach is a less invasive, more targeted alternative for treating radiation-sensitive tumors. A novel mechanophore-containing hydrogel...
This cancer treatment material and approach is a less invasive, more targeted alternative for treating radiation-sensitive tumors. A novel mechanophore-containing hydrogel is deposited at the tumor site and high-intensity focused ultrasound (HIFU) is used to locally generate cytotoxic reactive oxygen species (ROS) through an approach we call mechanochemical dynamic therapy (MDT). MDT dramatically decreases non-tumor cytotoxicity caused by conventional radiation treatments, which have to deliver damaging radiation through layers of healthy tissue to reach a tumor. Since HIFU can penetrate deep into and through tissues—including bone—MDT has the potential to significantly increase the number of tumors that are candidates for minimally invasive treatment. These combined features of targeted treatment (inaccessible through sonodynamic therapies) and the ability to treat deep-seated tumors (inaccessible through photodynamic therapy) makes MDT an extremely promising new approach for effective tumor treatment with minimal side effects.
Benefits:
Reduces side effects compared to photodynamic and sonodynamic therapies
