Synthesis and antitumor efficacy of a β-glucuronidase-responsive albumin-binding prodrug of doxorubicin.

Basic Information

ID: ALA2057162

Journal: J Med Chem

Title: Synthesis and antitumor efficacy of a β-glucuronidase-responsive albumin-binding prodrug of doxorubicin.

Authors: Legigan T, Clarhaut J, Renoux B, Tranoy-Opalinski I, Monvoisin A, Berjeaud JM, Guilhot F, Papot S.

Abstract: 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.

CiteXplore: 22515366

DOI: 10.1021/jm300348r

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