MEDI 338 |
| A new series of lipophilic camptothecin derivatives have been synthesized by attaching a cholesteryl group to camptothecin and camptothecin derivatives through a linker. The structure of new compounds has been characterized by 1H NMR, MS, FT-IR and elemental analysis. The new compounds are more soluble in biocompatible organic solvents such as soybean oil and vitamin E, and easily loaded into emulsion nanodroplets. In vitro cytotoxicty, as measured by GI50 values (50% of growth inhibition), of cholesterol-modified camptothecin compounds was investigated. The compounds with a cholesteryl group at C-10 show more anti-tumor effect, but those with a group at C-20 are less anti-tumor effect. It is interesting to note that the choice of linker had an effect on which cell types were most susceptible to our C-10 constructs. |
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Poster Session
7:00 PM-9:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster
Division of Medicinal Chemistry |