Bioorganic and Medicinal Chemistry Letters p. 1709 - 1714 (1997)
Update date:2022-08-11
Topics:
Marciano, Daniele
Aharonson, Ziporet
Varsano, Tal
Haklai, Roni
Kloog, Yoel
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.
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