Reaction of 2,3-dichloro-5,6-dicyano-benzoquinone (DDQ) with secondary enaminones yields surprisingly 2-aza-spiro[4,5]decatrienes. The reaction occurs via cyclisation of the primary Michael-adduct with the nitrile group. Reaction of DDQ with tertiary and also certain secondary enamines leads to 3-amino-benzo[b]furan derivatives. This is formed not by Michael-addition, but via geminate radical ion pair formation with subsequent generation of an oxygen-carbon bond to yield benzofurans. The new products are investigated with regards to inhibition of purified human proteinkinase CK2 and their general cytostatic activity. It turned out, that the most active compound is the 3-amino-5-hydroxy-benzofuran derivative 11s with an IC(50) value of 0,2μM for CK2.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmc.2011.03.006 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Insect farming: A bioeconomy-based opportunity to revalorize plastic wastes.
Environ Sci Ecotechnol
January 2025
Global Centre for Environmental Remediation (GCER), College of Engineering, Science and Environment, University of Newcastle, Callaghan, NSW, 2308, Australia.
Managing plastic waste is one of the greatest challenges humanity faces in the coming years. Current strategies-landfilling, incineration, and recycling-remain insufficient or pose significant environmental concerns, failing to address the growing volume of plastic residues discharged into the environment. Recently, increasing attention has focused on the potential of certain insect larvae species to chew, consume, and partially biodegrade synthetic polymers such as polystyrene and polyethylene, offering novel biotechnological opportunities for plastic waste management.
View Article and Find Full Text PDFLactate-induced protein lactylation in cancer: functions, biomarkers and immunotherapy strategies.
Front Immunol
January 2025
Department of Medical Laboratory, Affiliated Hospital of Jiujiang University, Jiujiang, Jiangxi, China.
Lactate, long viewed as a byproduct of glycolysis and metabolic waste. Initially identified within the context of yogurt fermentation, lactate's role extends beyond culinary applications to its significance in biochemical processes. Contemporary research reveals that lactate functions not merely as the terminal product of glycolysis but also as a nexus for initiating physiological and pathological responses within the body.
View Article and Find Full Text PDFPreparation and application of a multiepitope fusion protein based on bioinformatics and Tandem Mass Tag-based proteomics technology.
Front Immunol
January 2025
Jiangsu Engineering Research Center of Biological Data Mining and Healthcare Transformation, Xuzhou Medical University, Xuzhou, China.
Introduction: Brucellosis is a widespread zoonotic disease that poses a considerable challenge to global public health. Existing diagnostic methods for this condition, such as serological assays and bacterial culture, encounter difficulties due to their limited specificity and high operational complexity. Therefore, there is an urgent need for the development of enhanced diagnostic approaches for brucellosis.
View Article and Find Full Text PDFTuberculous meningitis diagnosis and treatment: classic approaches and high-throughput pathways.
Front Immunol
January 2025
Rehabilitation Medicine Department, The Affiliated Changsha Hospital of Xiangya School of Medicine, Central South University (The First Hospital of Changsha, Changsha, China.
Tuberculous meningitis (TBM), a severe form of non-purulent meningitis caused by (Mtb), is the most critical extrapulmonary tuberculosis (TB) manifestation, with a 30-40% mortality rate despite available treatment. The absence of distinctive clinical symptoms and effective diagnostic tools complicates early detection. Recent advancements in nucleic acid detection, genomics, metabolomics, and proteomics have led to novel diagnostic approaches, improving sensitivity and specificity.
View Article and Find Full Text PDFBioinformatic and biochemical analysis uncovers novel activity in the 2-ER subfamily of OYEs.
RSC Chem Biol
January 2025
Department of Chemistry, Emory University Atlanta GA 30322 USA
Members of the old yellow enzyme (OYE) family utilize a flavin mononucleotide cofactor to catalyze the asymmetric reduction of activated alkenes. The 2-enoate reductase (2-ER) subfamily are of particular industrial relevance as they can reduce α/β alkenes near electron-withdrawing groups. While the broader OYE family is being extensively explored for biocatalytic applications, oxygen sensitivity and poor expression yields associated with the presence of an Fe/S cluster in 2-ERs have hampered their characterization.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!