Van Driessche, Alexandra; Kocere, Agnese; Everaert, Hannelien; Nuhn, Lutz; Van Herck, Simon; Griffiths, Gareth; Fenaroli, Federico; De Geest, Bruno G. published the artcile< pH-Sensitive Hydrazone-Linked Doxorubicin Nanogels via Polymeric-Activated Ester Scaffolds: Synthesis, Assembly, and In Vitro and In Vivo Evaluation in Tumor-Bearing Zebrafish>, Formula: C9H3F5O2, the main research area is doxorubicin nanogel antitumor hydrazone tumor.
Nanoparticle conjugation is a powerful method to reduce the side effects of anticancer agents such as doxorubicin by altering the pharmacokinetic profile of the drug. Nanoparticles can prolong the circulation time and could also promote enhanced accumulation in tumors, either passively via the enhanced permeability and retention effect or actively when decorated with targeting motifs. For the particular case of doxorubicin, the hydrazone-based conjugation chem. is popular but commonly involves laborious chem. transformation steps. Here, we report on a straightforward route for the synthesis of hydrazone-based doxorubicin-polymer conjugates starting from a polymeric-activated ester scaffold onto which doxorubicin-reactive hydrazide moieties are introduced by simple treatment with hydrazine. Using block copolymers composed of a hydrophobic reactive ester block, we demonstrate a simple route to assemble core-crosslinked doxorubicin-loaded nanoparticles. The latter largely retain their bioactivity in vitro. In a zebrafish embryo “”premurine”” in vivo model, we demonstrate a drastic reduction in the systemic toxicity of doxorubicin upon nanoparticle conjugation and also demonstrate enhanced tumor accumulation and tumor growth reduction
Chemistry of Materials published new progress about Antitumor agents. 71195-85-2 belongs to class esters-buliding-blocks, and the molecular formula is C9H3F5O2, Formula: C9H3F5O2.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics