Ontology highlight
ABSTRACT:
SUBMITTER: Patil S
PROVIDER: S-EPMC4678411 | biostudies-literature | 2015 Dec
REPOSITORIES: biostudies-literature
Patil Satish S Lis Lev G LG Schumacher Robert J RJ Norris Beverly J BJ Morgan Monique L ML Cuellar Rebecca A D RA Blazar Bruce R BR Suryanarayanan Raj R Gurvich Vadim J VJ Georg Gunda I GI
Journal of medicinal chemistry 20151124 23
A disodium phosphonooxymethyl prodrug of the antitumor agent triptolide was prepared from the natural product in three steps (39% yield) and displayed excellent aqueous solubility at pH 7.4 (61 mg/mL) compared to the natural product (17 μg/mL). The estimated shelf life (t90) for hydrolysis of the prodrug at 4 °C and pH 7.4 was found to be two years. In a mouse model of human colon adenocarcinoma (HT-29), the prodrug administered intraperitoneally was effective in reducing or eliminating xenograf ...[more]