Synthesis and biological evaluation of glucuronide prodrugs of the histone deacetylase inhibitor CI-994 for application in selective cancer chemotherapy. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2008

Synthesis and biological evaluation of glucuronide prodrugs of the histone deacetylase inhibitor CI-994 for application in selective cancer chemotherapy.

Résumé

Two glucuronide prodrugs of the histone deacetylase inhibitor CI-994 were synthesized. These compounds were found to be soluble in aqueous media and stable under physiological conditions. The carbamoyl derivatisation of CI-994 significantly decreased its toxicity towards NCI-H661 lung cancer cells. Prodrug incubation with beta-glucuronidase in the culture media led efficiently to the release of the parent drug and thereby restoring its ability to decrease cell proliferation, to inhibit HDAC and to induce E-Cadherin expression.

Domaines

Cancer

Dates et versions

hal-00458881 , version 1 (22-02-2010)

Identifiants

Citer

Mickaël Thomas, Jonathan A. Clarhaut, Isabelle Tranoy-Opalinski, Jean-Pierre Gesson, Joëlle Roche, et al.. Synthesis and biological evaluation of glucuronide prodrugs of the histone deacetylase inhibitor CI-994 for application in selective cancer chemotherapy.. Bioorganic and Medicinal Chemistry, 2008, 16 (17), pp.8109-8116. ⟨10.1016/j.bmc.2008.07.048⟩. ⟨hal-00458881⟩

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