Articles publicats en revistes (Química Inorgànica i Orgànica)

deaths. The high mortality associated with CRC is attributed mainly to difficulties in early detection and lack of effective targeted therapies. The Transferrin receptor 1 (TfR1) is particularly attractive as a therapy target given its notable overexpression in tumor cells, particularly in CRC. This study explored the potential of a polymeric nanoparticle (PSomes)-based drug delivery system targeting TfR1 to improve the precision and efficacy of CRC treatment. For this study, we used two human CRC cell lines (HT-29, and HCT116), a healthy human intestinal epithelial cell line (hIECs), and a murine CRC cell line (MC38). We engineered PSomes composed of poly (ethylene glycol) (PEG) and poly (lactic acid) (PLA), functionalized with the T7 peptide to enhance their specificity for TfR1-expressing cells. Targeting efficiency of these PSomes was assessed across all cell lines by evaluating the cellular uptake using flow cytometry. Upon establishing the optimal formulation for these NPs for TfR1-targeting, we encapsulated doxorubicin (DOX) to assess their therapeutic potential. Both in vitro and in vivo experiments demonstrated that DOX loaded TfR1-targeted PSomes delivered DOX to CRC cells, leading to efficient induction of CRC cell death, reducing tumor growth and improving survival rates, compared to the control groups. These results highlight the promise of TfR1-targeted PSomes as a precise strategy for CRCtherapy, offering enhanced treatment efficacy while reducing systemic toxicity. This novel approach could lead to more targeted and less harmful cancer treatments.

monitor the binding. The binding affinity of PtL2 for MTOA·Cl is 2-fold smaller than that of the C[4]P precursor. This difference is attributed to dissimilar anion−π interactions and binding geometries in the ion-paired complexes of the two receptors, (Cl⊂PtL2/C[4]P)@MTOA. Isothermal titration calorimetry (ITC) experiments revealed subtle differences in enthalpy and entropy. The entropic term, although negative, was very small, suggesting the relevance of the dissociation/association processes of the salt and the ion-paired complexes. We investigated the binding selectivity of PtL2 toward a series of halides in acetone solution favoring ion-pair dissociation. PtL2 binds chloride selectively and with a high affinity, producing mainly an anionic complex.

Access to extended perylene-based nanographenes (NGs) is severely limited and involves tedious multi-step synthetic procedures. Here a two-step synthesis shortcut to highly soluble, bent, and extended perylene-based NGs from a nonperylene aromatic homologation precursor is reported. Moreover, the resulting scaffold, tetraphenyldibenzoperiflanthene (DBP), is further extended by Pd-based postsynthetic ring fusion, taking advantage of the installation of an aminoquinoline directing group. The rational extension of the DBP scaffold allows synthesizing of highly NIR

fluorescent pure-red emitters (λem > 700 nm) with excellent quantum yields (ΦFI) up to 0.78. Thorough theoretical analysis sheds light on the correlation between λem, ΦFI, and scaffold molecular editing and extension, showcasing a rational design evolution process toward NGs with desired photophysical properties.