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2005
Enzyme inhibiting activity
X 0220
Stable Propylphosphonic Acid Analogues of Geranylgeranyl Diphosphate PosInhibitory Activity on Geranylgeranyl Protein Transferase. — The origi15- 239 sessing
nal (phosphonoacetamido)oxy portion of the "short" lead compound, an analogue of
geranylgeranyl diphosphate, is elongated by introduction of an additional methylene
moiety. Within the methylene-elongated series the influence on the enzyme inhibitory
activity by introduction of a polar group as well as by removal of the linking oxygen
atom is examined. The new stable analogues, possessing 3-(phosphono)propionamido
moieties in place of the metabolically unstable diphosphate portion, are submitted to
prenyltransferase (GGTase and FTase) inhibition assays. In comparison with the "short"
lead, (Ia) shows an improved GGTase inhibitory activity but is less selective vs. FTase.
— (MACCHIA*, M.; et al.; Farmaco 59 (2004) 11, 857-861; Dip. Sci. Farm., Univ.
Pisa, I-56126 Pisa, Italy; Eng.) — H. Hoennerscheid
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