Towards the synthesis of new sequestring hexadentate bisphosphonic ligands for iron ion chelation

This work presents the design and the synthesis of precursors of hexadentate bisphosphonic ligands able to complex iron cation. This study describes coupling reaction between natural siderophore entity and bisphosphonic acids. These latter have properties of complexing heavy metals. These compounds were obtained from amidation reaction between a protected and activated bisphosphonic compound and serine trilactone. In the intermediate species, all the hydroxyl groups of phosphorus are esterified with ethyl group. The coupling method gave access to triserinelactone-bisphosphonate conjugates in good yields.</p

Synthesis and Antitumor Efficacy of a β-Glucuronidase-Responsive Albumin-Binding Prodrug of Doxorubicin

In this paper we describe the synthesis and biological evaluation of the first β-glucuronidase-responsive albumin-binding prodrug designed for the selective delivery of doxorubicin at the tumor site. This prodrug leads to superior antitumor efficacy in mice compared to HMR 1826, a well-known glucuronide prodrug of doxorubicin that cannot bind covalently to circulating albumin. Furthermore, this compound inhibits tumor growth in a manner similar to that of doxorubicin while avoiding side effects induced by the free drug