Mark J. Kurth
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Supplementary Figures 1-4, Methods from Halogenated Benzimidazole Carboxamides Target Integrin α<sub>4</sub>β<sub>1</sub> on T-Cell and B-Cell Lymphomas Open
Supplementary Figures 1-4, Methods from Halogenated Benzimidazole Carboxamides Target Integrin α4β1 on T-Cell and B-Cell Lymphomas
Supplementary Figures 1-4, Methods from Halogenated Benzimidazole Carboxamides Target Integrin α<sub>4</sub>β<sub>1</sub> on T-Cell and B-Cell Lymphomas Open
Supplementary Figures 1-4, Methods from Halogenated Benzimidazole Carboxamides Target Integrin α4β1 on T-Cell and B-Cell Lymphomas
Data from Halogenated Benzimidazole Carboxamides Target Integrin α<sub>4</sub>β<sub>1</sub> on T-Cell and B-Cell Lymphomas Open
Integrin α4β1 is an attractive but poorly understood target for selective diagnosis and treatment of T-cell and B-cell lymphomas. This report focuses on the rapid microwave preparation, structure-activity relationships, and biological eval…
Data from Halogenated Benzimidazole Carboxamides Target Integrin α<sub>4</sub>β<sub>1</sub> on T-Cell and B-Cell Lymphomas Open
Integrin α4β1 is an attractive but poorly understood target for selective diagnosis and treatment of T-cell and B-cell lymphomas. This report focuses on the rapid microwave preparation, structure-activity relationships, and biological eval…
Preparation of 3-Substituted Isoindolin-1-one, Cinnoline, and 1,2,4-[<i>e</i>]-Benzotriazine Derivatives Open
Herein, we report a new approach to synthesize a series of 1,2,4-[e]-benzotriazine and cinnoline derivatives from 3-substituted isoindolin-1-one. All the reported products are obtained through an economical two-step synthetic procedure res…
Autoimmunity affecting the biliary tract fuels the immunosurveillance of cholangiocarcinoma Open
Cholangiocarcinoma (CCA) results from the malignant transformation of cholangiocytes. Primary sclerosing cholangitis (PSC) and primary biliary cholangitis (PBC) are chronic diseases in which cholangiocytes are primarily damaged. Although P…
Heterocycles as a Peptidomimetic Scaffold: Solid-Phase Synthesis Strategies Open
Peptidomimetics are a privileged class of pharmacophores that exhibit improved physicochemical and biological properties. Solid-phase synthesis is a powerful tool for gaining rapid access to libraries of molecules from small molecules to b…
A Redox Isomerization Strategy for Accessing Modular Azobenzene Photoswitches with Near Quantitative Bidirectional Photoconversion Open
Photoswitches capable of accessing two geometric states are highly desirable, especially if their design is modular and incorporates a pharmacophore tethering site. We describe a redox isomerization strategy for synthesizing p-formylazoben…
Davis–Beirut Reaction: A Photochemical Brønsted Acid Catalyzed Route to <i>N</i>-Aryl 2<i>H</i>-Indazoles Open
The Davis-Beirut reaction provides access to 2H-indazoles from aromatic nitro compounds. However, N-aryl targets have been traditionally challenging to access due to competitive alternate reaction pathways. Previously, the key nitroso imin…
Davis–Beirut Reaction: Diverse Chemistries of Highly Reactive Nitroso Intermediates in Heterocycle Synthesis Open
Indazoles are an important class of nitrogen heterocycles because of their excellent performance in biologically relevant applications, such as in chemical biology and medicinal chemistry. In these applications, convenient synthesis using …
Accessing Multiple Classes of 2<i>H</i>-Indazoles: Mechanistic Implications for the Cadogan and Davis–Beirut Reactions Open
The Cadogan cyclization is a robust but harsh method for the synthesis of 2 H-indazoles, a valuable class of nitrogen heterocycles. Although nitrene generation by exhaustive deoxygenation is widely accepted as the operating mechanism in th…
Novel 2-(5-Imino-5<i>H</i>-isoquinolones[3,4-<i>b</i>]quinoxalin-7-ylmethyl)-benzonitrile (<b>DIQ3</b>) and Other Related Derivatives Targeting Colon Cancer Cells: Syntheses and in Vitro Models Open
Chemotherapy has been shown to be effective in reducing the progression and development of cancer in metastatic patients. However, drug selectivity is still a major issue for most chemotherapeutics. In this study, we synthesized four novel…
Photochemical Preparation of 1,2-Dihydro-3<i>H</i>-indazol-3-ones in Aqueous Solvent at Room Temperature Open
o-Nitrosobenzaldehyde is a reactive intermediate useful in the synthesis of nitrogen heterocycles. Previous strategies for using o-nitrosobenzaldehyde involve its isolation via chromatography and/or formation under harsh conditions. Herein…
CCDC 1871682: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
CCDC 1824483: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
CCDC 1824113: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
CCDC 1824115: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
CCDC 1856473: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
Diverting Reactive Intermediates Toward Unusual Chemistry: Unexpected Anthranil Products from Davis–Beirut Reaction Open
The discovery of a new variation on the Davis-Beirut reaction is described in which an atypical heterocyclic framework (the anthranil or benzo[c]isoxazole framework) is formed as the result of diversion of a key reactive intermediate away …
High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators Open
We previously identified phenylquinoxalinone CFTRact-J027 (4) as a cystic fibrosis transmembrane conductance regulator (CFTR) activator with an EC50 of ∼200 nM and demonstrated its therapeutic efficacy in mouse models of constipation. Here…
The fingerprint of antimitochondrial antibodies and the etiology of primary biliary cholangitis Open
The identification of environmental factors that lead to loss of tolerance has been coined the holy grail of autoimmunity. Our work has focused on the reactivity of antimitochondrial autoantibodies (AMA) to chemical xenobiotics and has hyp…
CCDC 1445328: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …