Novel inhibitors of the prenylated protein methyltransferase reveal distinctive structural requirements

D Marciano, Z Aharonson, T Varsano, R Haklai…

Index: Marciano, Daniele; Aharonson, Ziporet; Varsano, Tal; Haklai, Roni; Kloog, Yoel Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 13 p. 1709 - 1714

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Citation Number: 12

Abstract

Inhibitors of a prenylated protein methyltransferase were synthesized and evaluated. S- farnesyl-5-fluorothiosalicylic acid and the 5-chloro analog (but not the 4-fluoro, 4-chloro or 3- chloro analogs) were potent inhibitors, as was the parent compound S-farnesyl thiosalicylic acid (FTS), whose methyl ester was far less active. S-geranyl and S-geranylgeranyl thiosalicylic acids were more than ten times less potent than FTS.