Biological activity of PtIV prodrugs triggered by riboflavin-mediated bioorthogonal photocatalysis
AbstractWe have recently demonstrated that riboflavin (Rf) functions as unconventional bioorthogonal photocatalyst for the activation of PtIV prodrugs. In this study, we show how the combination of light and Rf with two PtIV prodrugs is a feasible strategy for light-mediated pancreatic cancer cell death induction. In Capan-1 cells, which have high tolerance against photodynamic therapy, Rf-mediated activation of the cisplatin and carboplatin prodrugs cis,cis,trans-[Pt(NH3)2(Cl)2(O2CCH2CH2CO2H)2] (1) and cis,cis,trans-[Pt(NH3)2(CBDCA)(O2CCH2CH2CO2H)2] (2, where CBDCA = cyclobutane dicarboxylate) resulted in pronounced reduction of the cell viability, including under hypoxia conditions. Such …
Ruthenium-arene complexes bearing naphthyl-substituted 1,3-dioxoindan-2-carboxamides ligands for G-quadruplex DNA recognition.
Quadruplex nucleic acids – DNA/RNA secondary structures formed in guanine rich sequences – proved to have key roles in the biology of cancers and, as such, in recent years they emerged as promising targets for small molecules. Many reports demonstrated that metal complexes can effectively stabilize quadruplex structures, promoting telomerase inhibition, downregulation of the expression of cancer-related genes and ultimately cancer cell death. Although extensively explored as anticancer agents, studies on the ability of ruthenium arene complexes to interact with quadruplex nucleic acids are surprisingly almost unknown. Herein, we report on the synthesis and characterization of four novel Ru(…
Catalysis Concepts in Medicinal Inorganic Chemistry
Catalysis has strongly emerged in the field of medicinal inorganic chemistry as a suitable tool to deliver new drug candidates and to overcome drawbacks associated to metallodrugs. In this Concept article, we discuss representative examples of how catalysis has been applied in combination with metal complexes to deliver new therapy approaches. In particular, we explain key achievements in the design of catalytic metallodrugs that damage biomolecular targets and in the development of metal catalysis schemes for the activation of exogenous organic prodrugs. Moreover, we discuss our recent discoveries on the flavin-mediated bioorthogonal catalytic activation of metal-based prodrugs; a new cata…
CCDC 1870492: Experimental Crystal Structure Determination
Related Article: Laura A. Hager, Stephan Mokesch, Claudia Kieler, Silvia Alonso-de Castro, Dina Baier, Alexander Roller, Wolfgang Kandioller, Bernhard K. Keppler, Walter Berger, Luca Salassa, Alessio Terenzi|2019|Dalton Trans.|48|12040|doi:10.1039/C9DT02078K
CCDC 1870494: Experimental Crystal Structure Determination
Related Article: Laura A. Hager, Stephan Mokesch, Claudia Kieler, Silvia Alonso-de Castro, Dina Baier, Alexander Roller, Wolfgang Kandioller, Bernhard K. Keppler, Walter Berger, Luca Salassa, Alessio Terenzi|2019|Dalton Trans.|48|12040|doi:10.1039/C9DT02078K
CCDC 1870493: Experimental Crystal Structure Determination
Related Article: Laura A. Hager, Stephan Mokesch, Claudia Kieler, Silvia Alonso-de Castro, Dina Baier, Alexander Roller, Wolfgang Kandioller, Bernhard K. Keppler, Walter Berger, Luca Salassa, Alessio Terenzi|2019|Dalton Trans.|48|12040|doi:10.1039/C9DT02078K