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

M Thomas, J Clarhaut, I Tranoy-Opalinski…

文献索引：Thomas, Mickael; Clarhaut, Jonathan; Tranoy-Opalinski, Isabelle; Gesson, Jean-Pierre; Roche, Joelle; Papot, Sebastien Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 17 p. 8109 - 8116

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被引用次数: 27

摘要

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 β-glucuronidase in the culture media led efficiently to the release of the parent drug and thereby restoring its ...