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Manuscript_Pavic et al_FZ_ESI.pdf (9.1 MB)

Highly Potent Rhenium(I) Tricarbonyl Complexes with Dual Anticancer and Anti-Angiogenic Activity Against Colorectal Carcinoma

preprint
revised on 25.03.2020, 15:09 and posted on 26.03.2020, 06:38 by Joachim Delasoie, Aleksandar Pavic, Noémie Voutier, Sandra Vojnovic, Aurélien Crochet, Jasmina Nikodinovic-Runic, Fabio Zobi
Synthesized and characterized a series of rhenium(I) trycarbonyl-based complexes with increased lipophilicity. Two of these novel compounds were discovered to possess remarkable anticancer, anti-angiogenic and antimetastatic activity in vivo (zebrafish-human CRC xenograft model), being effective at very low doses (1-3 µM). At doses as high as 250 µM the complexes did not provoke toxicity issues encountered in clinical anticancer drugs (cardio-, hepato-, and myelotoxicity). The two compounds exceed the antiproliferative and anti-angiogenic potency of clinical drugs cisplatin and sunitinib-malate, and display a large therapeutic window.

Funding

Bio-Inspired Vectors and Materials for the Targeted Delivery of CO-Releasing Molecules and Chemotherapeutic Agents - PP00P2_170589 - Swiss National Science Foundation

Ministry of Education, Science and Technological Development of the Republic of Serbia - Project No.173048

History

Email Address of Submitting Author

fabio.zobi@unifr.ch

Institution

Université de Fribourg

Country

Switzerland

ORCID For Submitting Author

0000-0002-9077-7184

Declaration of Conflict of Interest

No conflict of interest

Version Notes

Version Notes 1

Exports