Pyrano[3,2- c]pyridone and pyrano[3,2- c]quinolone structural motifs are commonly found in alkaloids manifesting diverse biological activities. As part of a program aimed at structural simplification of bioactive natural products utilizing multicomponent synthetic processes, we developed compound libraries based on these privileged heterocyclic scaffolds. The selected library members display low nanomolar antiproliferative activity and induce apoptosis in human cancer cell lines. Mechanistic studies reveal that these compounds induce cell cycle arrest in the G2/M phase and block in vitro tubulin polymerization. Because of the successful clinical use of microtubule-targeting agents, these heterocyclic libraries are expected to provide promising new leads in anticancer drug design.
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http://dx.doi.org/10.1021/jm701499n | DOI Listing |
Eur J Med Chem
January 2025
Laboratory of Medicinal Chemical Biology, Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Suzhou Medical College, Soochow University, 199 Ren'ai Road, Suzhou, 215123, PR China. Electronic address:
Pleurotin (1) is a benzoquinone meroterpenoid known for its wide-spectrum antitumor and antibiotic activities, notably acting as natural inhibitors of the thioredoxin reductase (TrxR). Pleurotin (1) has been chemically synthesized, but only in milligram quantities through at least 13 longest linear steps with 0.8 % overall yield due to its complex structure such as fused hexacyclic core with 8 contiguous stereocenters.
View Article and Find Full Text PDFJ Clin Med
January 2025
Department of Operative Gynecology, Federal State Budget Institution V. I. Kulakov Research Centre for Obstetrics, Gynecology, and Perinatology, Ministry of Health of the Russian Federation, 117997 Moscow, Russia.
: The diagnosis and treatment of endometriosis should be based on the best available evidence. Emphasising the risk of bias, the pyramid of evidence has the double-blind, randomised controlled trial and its meta-analyses on top. After the grading of all evidence by a group of experts, clinical guidelines are formulated using well-defined rules.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Medical Chemistry, Institute of Chemistry, Saint Petersburg State University, Saint Petersburg 199034, Russia.
The use of the concept of privileged structures significantly accelerates the search for new leads and their optimization. 6-(methylsulfonyl)-8-(4-methyl-4-1,2,4-triazol-3-yl)-2-(5-nitro-2-furoyl)-2,6-diazaspiro[3.4]octane has been identified as a lead, with MICs of 0.
View Article and Find Full Text PDFBMC Nurs
January 2025
The First Affiliated Hospital of China Medical University, No.155, Nanjing North Street, Heping District, Shenyang, Liaoning Province, China.
Background: Self-management is regarded as a crucial factor influencing the effectiveness of home-based cardiac rehabilitation for patients with coronary heart disease. In nursing practice, nurses employ a variety of strategies to enhance self-management of patients. However, there exists a disparity in nurses' perceptions and practical experiences with these strategies.
View Article and Find Full Text PDFViruses
December 2024
Centre for Outcomes Research and Evaluation, Research Institute of the McGill University Health Centre, Montreal, Canada.
Hepatitis C virus (HCV) disproportionately affects certain sub-populations, including people with experience of incarceration (PWEI). Little is known about how perceptions of HCV and treatment have changed despite simplifications in testing and treatment in carceral settings. Nineteen semi-structured interviews were conducted with people living with or having a history of HCV infection released from Quebec provincial prison.
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