Evaluation of Re(I) luminescent compounds in bio-imaging and/or antitumor agents

Abstract

The success of platinum-based anticancer drugs, in recent decades, has led to the development of other metallodrugs, which have been driven by the increased platinum resistance and its serious side effects associated with chemotherapy. In particular, the organometallic compounds of rhenium(I), fac-[Re(CO)3(NN)(L)]0/+, which are rapidly and efficiently up taken, with similar or superior activity to cisplatin and their toxicity were shown to be directly proportional to their lipophilicity. The great majority of rhenium compounds were initially used as luminescent sensors due to the intense 3MLCT emission, and their anticancer effect was only discovered during the biocompatibility screening. The present project aims to synthesize, characterize, investigate the luminescent properties of rhenium(I) compounds with NN ligands that have different chain conjugations and to establish a relationship between structure, lipophilicity and mechanisms of action in the cellular environment. To this, NN ligands and substituted pyridine L ligands will be used and should result in complexes with adequate characteristics with respect to solubility and photophysical properties to promote their use in bio-imaging and/or as therapeutic agents. The coordination of the different ligands is aimed to obtain complexes with high emission quantum yields as well as for the modulation/adjustment of lipophilicity characteristics. After complete characterization and study of photophysical properties in solution, investigations using different cells, such as breast cancer (MCF-7 and MCF-10-A) and blood cancer (leukemia), can be performed. (AU)