A set of novel hydrazone derivatives were synthesized and analyzed for their biological activities. The compounds were tested for their inhibitory effect on the phosphorylating activity of the protein kinase CK2, and their antioxidant activity was also determined in three commonly used assays. The hydrazones were evaluated for their radical scavenging against the DPPH, ABTS and peroxyl radicals. Several compounds have been identified as good antioxidants as well as potent protein kinase CK2 inhibitors. Most hydrazones containing a 4-N(CH ) residue or perfluorinated phenyl rings showed high activity in the radical-scavenging assays and possess nanomolar IC values in the kinase assays.
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http://dx.doi.org/10.1002/cmdc.202100047 | DOI Listing |
Pharmaceuticals (Basel)
January 2025
Centro de Química Estrutural, Institute of Molecular Sciences, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.
Background/objectives: Cancer remains one of the major challenges of our century. Organometallic ruthenium complexes are gaining recognition as a highly promising group of compounds in the development of cancer treatments.
Methods: Building on the auspicious results obtained for [Ru(η-CH)(PPh)(bipy)][CFSO] (TM34), our focus has shifted to examining the effects of incorporating bioactive ligands into the TM34 framework, particularly within the cyclopentadienyl ring.
Molecules
January 2025
College of Chemistry and Chemical Engineering, Taiyuan University of Technology, Taiyuan 030024, China.
A series of novel triazone derivatives containing aldehyde hydrazone or ketone hydrazone moieties were designed, synthesized and their biological activities were investigated against , , , , and 14 Kinds of fungi. Most of the aldehyde hydrazone exhibited excellent insecticidal activities against . In particular, the aphicidal activities of compounds (35%) and (30%) were equivalent to pymetrozine (30%) at 5 mg/kg.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
State Key Laboratory of Green Pesticides, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China. Electronic address:
As the vital the biomacromolecule in eukaryotic cells, tubulin protein is essential for preserving cell shape, facilitating cell division, and cell viability. Tubulin has been approved as promising target for anticancer, and antifungal therapy. However, there are still many gaps in tubulin-targeted fungicidal discovery.
View Article and Find Full Text PDFJ Fungi (Basel)
January 2025
Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, Brazil.
Fungal infections have become a growing concern in healthcare, particularly in immunocompromised individuals, with species like , , and posing significant challenges due to rising resistance and limited treatment options. In response, novel antifungal agents are being explored, including thiazolyl hydrazones. This study focuses on the development of a novel thiazolylhydrazone derivative, RW3.
View Article and Find Full Text PDFJ Inorg Biochem
January 2025
Department of Chemistry, Karpagam Academy of Higher Education, Coimbatore 641 021, India; Centre for Material Chemistry, Karpagam Academy of Higher Education (Deemed to be University), Coimbatore 641 021, India. Electronic address:
A series of new Pd(II) complexes were synthesized from the reaction of andrographolide appended hydrazide derivatives with potassium tetrachloropalladate K[PdCl]. The formation of the complexes was confirmed through structural assessments conducted using various spectroscopic techniques. From the spectral studies we confirmed that the ligands coordinated to Pd(II) ion via amine nitrogen and enone oxygen.
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