Synthesis of acyloxymethyl ester prodrugs of the transferable protein farnesyl transferase substrate farnesyl methylenediphosphonate |
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| Authors: | Troutman Jerry M Chehade Kareem A H Kiegiel Katarzyna Andres Douglas A Spielmann H Peter |
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| Institution: | Department of Molecular and Cellular Biochemistry, University of Kentucky, Lexington, KY 40536-0084, USA. |
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| Abstract: | Three isoprenoid diphosphate analogues of farnesyl diphosphate (FPP) where the diphosphate has been replaced by methylene diphosphonate and the negative charges masked by frangible pivaloyloxymethyl (POM) esters were prepared. Farnesyl methylenediphosphonate is a sub-micromolar substrate for protein farnesyl transferase. The tripivaloyloxymethyl esters of isoprenoid methylenediphosphonate have significantly increased lipophilicity and may act as important farnesyl diphosphate prodrugs. |
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