0000000001302962
AUTHOR
Dina Baier
Targeting a Targeted Drug: An Approach Toward Hypoxia-Activatable Tyrosine Kinase Inhibitor Prodrugs
Tyrosine kinase inhibitors (TKIs), which have revolutionized cancer therapy over the past 15 years, are limited in their clinical application due to serious side effects. Therefore, we converted two approved TKIs (sunitinib and erlotinib) into 2-nitroimidazole-based hypoxia-activatable prodrugs. Kinetics studies showed very different stabilities over 24 h; however, fast reductive activation via E. coli nitroreductase could be confirmed for both panels. The anticancer activity and signaling inhibition of the compounds against various human cancer cell lines were evaluated in cell culture. These data, together with molecular docking simulations, revealed distinct differences in the impact of …
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(…
124I Radiolabeling of a AuIII‐NHC Complex for In Vivo Biodistribution Studies†
Abstract AuIII complexes with N‐heterocyclic carbene (NHC) ligands have shown remarkable potential as anticancer agents, yet their fate in vivo has not been thoroughly examined and understood. Reported herein is the synthesis of new AuIII‐NHC complexes by direct oxidation with radioactive [124I]I2 as a valuable strategy to monitor the in vivo biodistribution of this class of compounds using positron emission tomography (PET). While in vitro analyses provide direct evidence for the importance of AuIII‐to‐AuI reduction to achieve full anticancer activity, in vivo studies reveal that a fraction of the AuIII‐NHC prodrug is not immediately reduced after administration but able to reach the major…
CCDC 1989307: Experimental Crystal Structure Determination
Related Article: Federica Guarra, Alessio Terenzi, Christine Pirker, Rossana Passannante, Dina Baier, Ennio Zangrando, Vanessa G��mez���Vallejo, Tarita Biver, Chiara Gabbiani, Walter Berger, Jordi Llop, Luca Salassa|2020|Angew.Chem.,Int.Ed.|59|17130|doi:10.1002/anie.202008046
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 1989306: Experimental Crystal Structure Determination
Related Article: Federica Guarra, Alessio Terenzi, Christine Pirker, Rossana Passannante, Dina Baier, Ennio Zangrando, Vanessa G��mez���Vallejo, Tarita Biver, Chiara Gabbiani, Walter Berger, Jordi Llop, Luca Salassa|2020|Angew.Chem.,Int.Ed.|59|17130|doi:10.1002/anie.202008046
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