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In order to find multifunction anticancer complexes, three Mn(II) complexes of N-substituted di(2-pyridylmethyl)amine were characterized and used as agents to interfere with the functions of mitochondria and the metabolite of O(2) in cancer cells. It was found that carboxylate-bridged dimanganese(II) systems are good models of catalase and exhibit good inhibition of the proliferation of U251 and HeLa cells. The inhibiting activity of these manganese(II) complexes on the tumor cells in vitro was related to their disproportionating H(2)O(2) activity. The reaction of carboxylate-bridged dimanganese Mn(II) complex with H(2)O(2) forms a stable Mn(III)-(μ-O)(2)-Mn(IV) complex. Extensive experimental results show that chloride-bridged dimanganese(II) complexes could inhibit the swelling of calcium(II) overloaded mitochondria, and carboxylate-bridged manganese(II) complexes enhance the swelling of calcium(II) overloaded mitochondria. These results indicate that the interactions between Mn(II) complexes of N-substituted di(picolyl)amine and mitochondria are influenced by the structure and conformation of the complexes. Mn(II) complexes of N-substituted di(picolyl)amine could be developed as multifunctional anticancer complexes to interfere with the absorption of calcium(II) in mitochondria and the metabolite of O(2) through the H(2)O(2) or ROS involved signaling induced apoptosis of cancer cells.
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http://dx.doi.org/10.1021/ic200004y | DOI Listing |
Angew Chem Int Ed Engl
August 2025
Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CiQUS) and Departamento de Química Orgánica, Universidade de Santiago de Compostela, Santiago de Compostela, 15782, Spain.
An iridium complex featuring the perfluorinated bisphosphine ligand dppe can catalyze intermolecular hydrocarbonation reactions of allenes with precise control over the selectivity to yield highly valuable branched products instead of the more common linear derivatives. Using N-substituted 3-carboxamide pyrroles as C─H donors, the reaction gives exclusively C-4 substituted products, while furan analogues yield C-2 substituted derivatives. β-Unsubstituted acrylamides can also be used as C─H sources to give chiral skipped dienes.
View Article and Find Full Text PDFJ Am Chem Soc
August 2025
Borch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, 575 West Stadium Avenue, West Lafayette, Indiana 47907, United States.
Ligand discovery of nonenzymatic proteins can be accomplished through screening methods utilizing libraries comprising small molecules, peptides, and peptidomimetics. Incorporating peptoids, which are oligomers of -substituted glycine monomers, into high-throughput screens can produce libraries of large structural diversity. Due to their malleable structures, peptoids can occupy unique protein binding sites, but determination of the peptoid binding pose is challenging.
View Article and Find Full Text PDFOrg Lett
July 2025
Department of Chemistry, Bar-Ilan University, Ramat-Gan, 52900, Israel.
We report a mild, metal-free synthesis of 2,5-disubstituted thiazoles from readily available N-substituted α-amino acids. The reaction proceeds via carboxylic acid activation with thionyl chloride, followed by intramolecular cyclization and in situ sulfoxide deoxygenation, affording the target thiazoles in excellent yields. This transition-metal-free, robust, and scalable protocol enables access to a broad range of 2,5-disubstituted thiazoles, bypassing the need for complex reagents and significantly simplifying their synthesis.
View Article and Find Full Text PDFRSC Adv
May 2025
Chemistry Department, Faculty of Science, Mansoura University Mansoura 35516 Egypt +20-1093427024.
This review discusses the significant advances in the current status and latest synthesis techniques for -substituted 3-acetyl-4-hydroxyquinolinones. They are an important class of alkaloids possessing different electrophilic and nucleophilic centers. In this review, we comprehensively summarize the synthesis of 3-acetylquinolones various reactions, emphasizing recent developments and challenges.
View Article and Find Full Text PDFJ Inorg Biochem
October 2025
Schulich Faculty of Chemistry, Technion-Israel Institute of Technology Technion City, Haifa 3200008, Israel. Electronic address:
Peptoids (N-substituted glycine oligomers) represent an excellent platform for drug development, such as selective chelators for Cu ions towards chelation therapy, due to their efficient synthesis, high stability and good bioavailability. We previously showed that peptoids helicity is essential for selective Cu binding and identified a unique peptoid hexamer, having 2,2':6',2″-terpyridine, and 8-hydroxyquinoline as metal-binding sidechains facing the same side of the helix, which exhibits high selectivity to Cu ions. However, maintaining a stable helix required the incorporation of bulky chiral sidechains, resulting in a hydrophobic peptoid, insoluble in aqueous solutions, and limited in its use as a drug candidate.
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