Gene interactions and pathways from curated databases and text-mining
Bioorg Med Chem 2008, PMID: 18692397

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

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.