1075719-58-2Relevant academic research and scientific papers
Synthesis and biological evaluation of glucuronide prodrugs of the histone deacetylase inhibitor CI-994 for application in selective cancer chemotherapy
Thomas, Mickael,Clarhaut, Jonathan,Tranoy-Opalinski, Isabelle,Gesson, Jean-Pierre,Roche, Joelle,Papot, Sebastien
, p. 8109 - 8116 (2008/12/23)
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 ability to decrease cell proliferation, to inhibit HDAC and to induce E-Cadherin expression.
