Abstract
AbstractTwo new Drug Delivery Systems (DDS) cyclo[DKP‐isoDGR]‐PEG‐4‐Val‐Ala‐PTX (2) and cyclo[DKP‐isoDGR]‐PEG‐4‐sC18‐Val‐Ala‐PTX (3), containing the cyclo[DKP‐isoDGR] integrin ligand and the cytotoxic agent Paclitaxel (PTX), were synthesized to investigate the influence of a PEG‐4 chain and of the sC18 cell‐penetrating peptide (CPP) on the cellular uptake and the cytotoxicity of the constructs. A “double click‐reaction strategy” was planned, to realize the connection of cyclo[DKP‐isoDGR] and PTX to the CPP moiety. Anti‐proliferative bioassays were performed on the αVβ3‐positive U87 human glioblastoma cell line using a short contact time (15 min) followed by draining, washing of the cells, and re‐incubation for 72 h. Compound 3 was significantly more potent (IC50=27.6 μM) than compound 2 (IC50>100 μM), and showed a reduced potency loss with respect to PTX (IC50=71 nM).
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