Bioorg Med Chem 2008,
PMID: 18692397
Thomas, Mickaël; Clarhaut, Jonathan; Tranoy-Opalinski, Isabelle; Gesson, Jean-Pierre; Roche, Joëlle; Papot, Sébastien
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.
Diseases/Pathways annotated by Medline MESH: Lung Neoplasms
Document information provided by NCBI PubMed
Text Mining Data
E-Cadherin → HDAC: "
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
"
Manually curated Databases
No curated data.