15 research outputs found
Detection of cardioactivity in marine natural products using the frog heart assay
Thesis (B.S.) in Chemistry--University of Illinois at Urbana-Champaign, 1985.Bibliography: leaves 29-30.U of I OnlyTheses restricted to UIUC community onl
Amination of Nitro-Substituted Heteroarenes by Nucleophilic Substitution of Hydrogen
An open-air method for the transition metal-free direct amination of nitro(hetero)arenes by anilines is disclosed. In this methodology, an aromatic C-H bond is substituted via oxidative nucleophilic aromatic substitution of hydrogen (ONSH). DFT calculations and mechanistic studies support a dianion pathway with oxidation by molecular oxygen as the rate-limiting step
Discovery of Potent Heterodimeric Antagonists of Inhibitor of Apoptosis Proteins (IAPs) with Sustained Antitumor Activity
The
prominent role of IAPs in controlling cell death and their
overexpression in a variety of cancers has prompted the development
of IAP antagonists as potential antitumor therapies. We describe the
identification of a series of heterodimeric antagonists with highly
potent antiproliferative activities in cIAP- and XIAP-dependent cell
lines. Compounds <b>15</b> and <b>17</b> further demonstrate
curative efficacy in human melanoma and lung cancer xenograft models
and are promising candidates for advanced studies
Evolution of a Scale-Up Synthesis to a Potent GluN2B Inhibitor and Its Prodrug
This paper describes the efficient
scale-up synthesis of the potent
negative allosteric glutamate N2B (GluN2B) inhibitor <b>1</b> (BMS-986169), which relies upon a stereospecific S<sub>N</sub>2
alkylation strategy and a robust process for the preparation of its
phosphate prodrug <b>28</b> (BMS-986163) from parent <b>1</b> using POCl<sub>3</sub>. A deoxyfluorination reaction employing bis(2-methoxyethyl)aminosulfur
trifluoride (Deoxo-Fluor) is also used to stereospecifically introduce
a fluorine substituent. The optimized routes have been demonstrated
to provide APIs suitable for toxicological studies in vivo
Discovery of Potent Heterodimeric Antagonists of Inhibitor of Apoptosis Proteins (IAPs) with Sustained Antitumor Activity
The
prominent role of IAPs in controlling cell death and their
overexpression in a variety of cancers has prompted the development
of IAP antagonists as potential antitumor therapies. We describe the
identification of a series of heterodimeric antagonists with highly
potent antiproliferative activities in cIAP- and XIAP-dependent cell
lines. Compounds <b>15</b> and <b>17</b> further demonstrate
curative efficacy in human melanoma and lung cancer xenograft models
and are promising candidates for advanced studies