Abstract by David Wilcox
Chemistry and Biochemistry
Englerin: A Potential Drug Against Kidney Cancer
Englerin A is a potent anti-cancer compound derived from the bark of the East African shrub Phyllanthus engleri. It shows micromolar potency against most cancers and is especially effective against kidney cancer, with a GI50 of less than 20nM for renal cell carcinoma (RCC) cell lines. Although several labs have accomplished the total synthesis of Englerin A, the procedures are lengthy and expensive. As a simpler alternative, the Andrus lab hopes to produce an analog of Englerin A that can be used as new, selective RCC drug. The proposed analog replaces Englerin's five-membered ring with an isopropyl group. Molecular modeling calculations have confirmed that the change will keep the biologically active part of Englerin nearly perfectly intact. The proposed synthesis reduces the number of steps from over 15 to 9, making it an attractive alternative as a potential anti-cancer drug.