Less toxic chemotherapy with palladium
Dr Enrica Bortolamiol, Ca’ Foscari University of Venice; Prof. Flavio Rizzolio, Ca’ Foscari University of Venice; Prof. Fabiano Visentin, Ca’ Foscari University of Venice; Dr Thomas Scattolin, Ca’ Foscari University of Venice
Ca’ Foscari University of Venice
Chemotherapy has been using platinum-based antineoplastic drugs since the late 1970s, in spite of significant nephro- and neurotoxicity. Research in the field has been directed at testing the potentiality of compounds based on other transition metals.
Targeted, efficient and non-toxic anti-cancer drugs: Researchers from Ca’ Foscari University of Venice have synthesized an innovative and rare class of palladium(I) compounds, unexpectedly stable notwithstanding their unusual oxidation state of the metal. The research group tested them as anti-proliferating agents on some of the most aggressive tumors, such as ovarian, cervical, colon and lung cancers, achieving very promising results. In fact, the high cytotoxic effects on cancer cells accompanies a poor toxicity on cells extracted from healthy tissues, limiting the typical side effects of current treatments with cisplatin or related compounds.
Ca’ Foscari University seeks industrial partners for further development. The invention is offered for licensing or for sale.
The platinum-based antineoplastic drugs were tested in vitro (cell lines and tumoroids). The drugs show a high antiproliferative activity toward all tested cancer cell lines (A2780, A2780cis, OVCAR5, OVCAR3, KURAMOCHI and HeLa) and low toxicity toward normal cells (MRC-5 human lung fibroblasts).
PCT patent application Nr. PCT/EP2020/084360 filed on December 3, 2020
(Priority Italian patent application filed on December 2019).
- T. Scattolin, E. Bortolamiol, S. Palazzolo, I. Caligiuri, T. Perin, V. Canzonieri, N. Demitri, F. Rizzolio, L. Cavallo, B. Dereli, M. Mane, S. P. Nolan and F. Visentin, “The anticancer activity of an air-stable Pd(I)-NHC (NHC = N-heterocyclic carbene) dimer”. Chem. Commun. (2020), DOI: 10.1039/D0CC03883K.
- T. Scattolin , I. Caligiuri , N. Mouawad , M. El Boustani , N. Demitri , F. Rizzolio, F. Visentin. "Synthesis and in-depth studies on the anticancer activity of novelpalladacyclopentadienyl complexes stabilized by N-Heterocyclic carbene ligands". Eur. J. Med. Chem (2019) 179: 325-334.
- T. Scattolin , L. Canovese , N. Demitri, R. Gambari, I. Lampronti, C. Santo , F. Rizzolio, I. Caligiuri. F. Visentin. “Synthesis of new allyl palladium complexes bearing purine-based NHC ligands with antiproliferative and proapoptotic activity on human ovarian cancer cell lines“. Dalton Trans (2018) 47: 13616.