960214-87-3Relevant academic research and scientific papers
Podophyllotoxin analogues active versus Trypanosoma brucei
Uddin, Md. Jashim,Smithson, David C.,Brown, Kristin M.,Crews, Brenda C.,Connelly, Michele,Zhu, Fangyi,Marnett, Lawrence J.,Guy, R. Kiplin
supporting information; experimental part, p. 1787 - 1791 (2010/08/06)
In an effort to discover novel anti-trypanosomal compounds, a series of podophyllotoxin analogues coupled to non-steroidal anti-inflammatory drugs (NSAIDs) has been synthesized and evaluated for activity versus Trypanosoma brucei and a panel of human cell lines, revealing compounds with low nano-molar potencies. It was discovered that coupling of NSAIDs to podophyllotoxin increased the potencies of both compounds over 1300-fold. The compounds were shown to be cytostatic in nature and seem to act via de-polymerization of tubulin in a manner consistent with the known activities of podophyllotoxin. The potencies against T. brucei correlated directly with Log P values of the compounds, suggesting that the conjugates are acting as hydrophobic tags allowing podophyllotoxin to enter the cell.
