Bioorganic & medicinal chemistry

Synthesis and evaluation of homofarnesoyl-substituted CAAX-peptidomimetics as farnesyltransferase inhibitors and antiproliferative agents

M Schlitzer, I Sattler, HM Dahse

Index: Schlitzer, Martin; Sattler, Isabel; Dahse, Hans-Martin Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 9 p. 2037 - 2045

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Citation Number: 5

Abstract

Several CAAX-peptidomimetics were linked to homofarnesoic acid via a β-alanyl spacer with the intention to obtain a novel type of bisubstrate analogue farnesyltransferase inhibitors. However, the compounds were found to be only weakly active in the farnesyltransferase inhibition assay. Nevertheless, they displayed antiproliferative activity against different tumor cell lines in the low micromolar range. Replacement of the β- ...