A cobalt-catalyzed C2-selective amidation of indoles using acyl azides has been accomplished. Isotope experiments suggest that C-H activation is reversible. The use of sustainable Co catalysis, functional group diversity, substrate scope, and regioselectivity are the important practical features.
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http://dx.doi.org/10.1021/acs.joc.9b02244 | DOI Listing |
Chem Asian J
January 2025
National Institute of Technology Warangal, Department of Chemistry, Hanamkonda, 506004, Warangal, INDIA.
We report CBr4 catalyzed Michael addition of indole to α,β-unsaturated ketones for the synthesis of β-indolylketones through halogen bonding catalysis. This reaction is compatible with a diverse range of chalcones, including drug-derived chalcones containing sensitive functional groups such as amides, yielding the addition products in good yields. Additionally, 3-indolyl furanoid motifs have been synthesized through the Michael addition followed by Paal-Knorr cyclization by utilizing various unsymmetrical 1,4-enediones in a one-pot process with good yields.
View Article and Find Full Text PDFIntegr Cancer Ther
January 2025
Seoul Korean Medicine Hospital of Daejeon University, Seoul, Republic of Korea.
In this study, we investigated the synergistic effect of co-administration of osimertinib and HAD-B1 using gefitinib-resistant non-small cell lung cancer cells, HCC827-GR. HAD-B1 is composed of 4 natural drugs, Panax Notoginseng Radix, Panax ginseng C. A.
View Article and Find Full Text PDFMed
January 2025
Division of Neuro-Oncology, Stanford University, Stanford, CA 94305, USA; Department of Neurology and Neurological Sciences, Stanford University, Stanford, CA 94305, USA. Electronic address:
The phase III EVEREST trial evaluating zorifertinib in the treatment of metastatic EGFR-mutant NSCLC was groundbreaking in its specific inclusion of patients with brain metastases. Zorifertinib prolonged systemic and intracranial progression-free survival compared with first-generation EGFR inhibitors, yet questions remain about its efficacy and toxicity compared with osimertinib.
View Article and Find Full Text PDFMolecules
December 2024
Ufa Institute of Chemistry, Ufa Federal Research Centre, Russian Academy of Science, 71, Prospect Octyabrya, Ufa 450054, Russia.
Alzheimer's disease (AD) poses a significant public health issue. Despite the fact that today there are several methods of maintenance therapy, one of the most widely used methods is designed to correct the deficiency of acetylcholine. In the search for new potential inhibitors of cholinesterase enzymes, eight new derivatives of 3-oxo- or 2,3-indolo-triterpenic acid conjugated with amino-quinuclidine bicyclic cores were designed and synthesized.
View Article and Find Full Text PDFJ Cancer Res Ther
December 2024
Department of Oncology, The First Affiliated Hospital of Shandong First Medical University and Shandong Provincial Qianfoshan Hospital, Shandong Lung Cancer Institute, Shandong, China.
Osimertinib, a third-generation epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI), has revolutionized one of the standard most efficient treatments for EGFR mutation-positive non-small cell lung cancer (NSCLC). Osimertinib, a third-generation EGFR-TKI, is currently one of most efficient treatments in clinical practice. However, it has a potentially fatal side effect: interstitial lung disease (ILD).
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