Novel platinum(IV) coordination compounds with 5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7(4H)-one (HmtpO): cis-trans-[PtCl(2)(OH)(2)(NH(3))(HmtpO)] (1), cis-trans-[PtCl(5)(HmtpO)][(CH(3))(2)NH(2)] (2) have been prepared and structurally characterized by spectroscopic methods ((1)H, IR and X-ray crystallography (2)). The X-ray results indicate that the local geometry around the platinum(IV) centre approximates a typical octahedral arrangement with nitrogen atom N3 of the HmtpO and three chloride atoms in equatorial positions. The remaining two axial positions are occupied by two chlorides. The preliminary assessment of antitumor properties of (1) was performed as an in vitro antiproliferative activity against HL-60 human acute promyelocytic leukemia and HCV29T bladder cancer. The cis-trans-[PtCl(2)(OH)(2)(NH(3))(HmtpO)] (1) exhibits higher cytotoxic activity against HL-60 (IC(50)=6.4 μM) than cisplatin.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.saa.2011.03.019 | DOI Listing |
JACS Au
January 2025
School of Chemistry and Chemical Engineering, Chemistry and Biomedicine Innovation Center (ChemBIC), State Key Laboratory of Coordination Chemistry, Najing University, Nanjing 210023, PR China.
Cancer cells often upregulate ribosome biogenesis to meet increased protein synthesis demands for rapid proliferation; therefore, targeting ribosome biogenesis has emerged as a promising cancer therapeutic strategy. Herein, we introduce two Pt complexes, ataluren monosubstituted platinum(IV) (SPA, formula: c,c,t,-[Pt(NH)Cl(OH)(CHFNO)], where CHFNO = ataluren) and ataluren bisubstituted platinum(IV) complex (DPA, formula: c,c,t,-[Pt(NH)Cl(CHFNO)], where CHFNO = ataluren), which effectively suppress ribosome biogenesis by inhibiting 47s pre-RNA expression. Furthermore, SPA and DPA induce nucleolar stress by dispersing nucleolar protein NPM1, ultimately inhibiting protein generation in tumor cells.
View Article and Find Full Text PDFBiomed Pharmacother
January 2025
Czech Academy of Sciences, Institute of Biophysics, Kralovopolska 135, Brno CZ-61200, Czech Republic; Department of Biophysics, Faculty of Science, Palacky University, Slechtitelu 27, Olomouc 783 71, Czech Republic. Electronic address:
Platinum(IV) compounds possess distinct properties that set them apart from platinum(II) compounds. Often designed as prodrugs, they are reduced within cancer cells to their active platinum(II) form, enabling their cytotoxic effects. Their versatility also lies in their ability to be functionalized and conjugated with bioactive molecules to enhance cancer cell targeting.
View Article and Find Full Text PDFInorg Chem Front
January 2025
Center for Cancer Research and Comprehensive Cancer Center, Medical University of Vienna Borschkegasse 8a 1090 Vienna Austria +43 (0)1 40160-57557.
Platinum chemotherapy is part of every second anticancer treatment regimen. However, its application is limited by severe side effects and drug resistance. The combination of platinum-based chemotherapeutics with EGFR inhibitors has shown remarkable synergism in clinical treatment.
View Article and Find Full Text PDFDalton Trans
January 2025
Department of Chemistry, Babeş-Bolyai University, Str. Arany Janos Nr. 11, RO-400028 Cluj-Napoca, Romania.
The synthesis and characterization of novel platinum(II) and platinum(IV) complexes derived from unsymmetrical ethylene or propylenediamine derivatives are presented. IR spectroscopy and ESI mass spectrometry techniques were employed to characterize the complexes, revealing distinctive absorption bands and isotope patterns. Furthermore, the complexes were characterized by H and C NMR spectroscopy.
View Article and Find Full Text PDFJ Am Chem Soc
December 2024
Department of Chemistry, Brandon University, 270 18th Street, Brandon, Manitoba R7A 6A9, Canada.
Aerobic oxidation of a dimethylplatinum(II) complex featuring 1,1-di(2-pyridyl)ethanol as a supporting ligand leads to the formation of two unexpected Pt complexes (in ∼1:1 ratio), neither of which results from direct oxidation typical for Pt centers supported by popular κ-(,) ligands. While one product features an isomerized Pt center stabilized by the κ-(,,) ligand coordination mode, surprisingly, the other product results from intramolecular activation of the ligand methyl fragment. Mechanistic studies, reactivity of model complexes, and DFT calculations reveal that the critical proton-responsive nature of the ligand allows formation of intermediates that result in a concerted metalation deprotonation (CMD)-like C-H activation at Pt.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!