A new Heck-type reaction for the synthesis of chalcones has been established using Mannich bases as enone precursors. The novel reaction proceeds rapidly in air atmosphere under ligandless conditions and can be adapted for library synthesis in a parallel reactor station. Screening of the synthesized chalcones revealed N-{4-[(1E)-3-oxo-3-(3-pyridinyl)-1-propenyl]phenyl}benzamide (3f) to be a potent anti-leishmanial agent.
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http://dx.doi.org/10.1016/j.bmcl.2008.01.112 | DOI Listing |
Biomedicines
December 2024
Departamento de Ciência Básica, Instituto de Saúde de Nova Fribrugo, Universidade Federal Fluminense, Nova Friburgo 28625-650, RJ, Brazil.
Pyruvate kinase M2, a central regulator of cancer cell metabolism, has garnered significant attention as a promising target for disrupting the metabolic adaptability of tumor cells. This study explores the potential of the Mannich base derived from lawsone () to interfere with PKM2 enzymatic activity both in vitro and in silico. The antiproliferative potential of was tested using MTT assay in various cell lines, including SCC-9, Hep-G2, HT-29, B16-F10, and normal human gingival fibroblast (HGF).
View Article and Find Full Text PDFInorg Chem
December 2024
MTA-SZTE Lendület Functional Metal Complexes Research Group, University of Szeged, Dóm tér 7-8, Szeged H-6720 , Hungary.
Drug resistance is a major obstacle in cancer treatment. Herein, four novel organometallic complexes, with the general formula [Ru(η--cymene)(HL)Cl]Cl and [Rh(η-CMe)(HL)Cl]Cl, were developed to target multidrug-resistant (MDR) cancer cells, where HL denotes 8-hydroxyquinoline-derived Mannich bases (HQCl-pyr and HQCl-pip). The aim of the complexation was to obtain compounds with improved drug-like properties.
View Article and Find Full Text PDFFree Radic Res
November 2024
Faculty of Chemistry, Belarusian State University, Minsk, Belarus.
Free radicals are ubiquitous in biological systems, being responsible for pathogenesis of degenerative diseases and participating in vitally important biochemical processes, which are mediated by radical regulatory agents. The effects of the aliphatic amine substituents in the catechol-derived Mannich bases on their antioxidant and pro-oxidant activity were investigated. It has been found that the presence of catechol moiety in the structure of Mannich bases allows them to act as Cu(II) reductants, efficient Fe(II) chelators and potent DPPH radical scavengers.
View Article and Find Full Text PDFChemMedChem
November 2024
Department of Chemistry of Bioactive Nitrogen-Containing Heterocyclic Bases, V. P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine, Academika Kukharya Str. 1, 02094, Kyiv, Ukraine.
Chem Biodivers
November 2024
State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin, 300071, China.
Compounds containing N-pyridylpyrazole motif have aroused interest and brought about research hotspots due to their highly-efficient insecticidal activity. The fungicidal potential of N-pyridylpyrazole derivatives has gradually been disclosed in recent years. To discover new agrochemicals with poly-heterocyclic features, a series of novel triazole thione/thioether derivatives containing pyridylpyrazole motif (8-11) was synthesized.
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