TY - JOUR
T1 - Novel inhibitors of the prenylated protein methyltransferase reveal distinctive structural requirements
AU - Marciano, Daniele
AU - Aharonson, Ziporet
AU - Varsano, Tal
AU - Haklai, Roni
AU - Kloog, Yoel
N1 - Funding Information:
in part by the SAFAHO Foundation.
Funding Information:
This work was supported by a grant from the Israel Science Foundation 646196-16.1
PY - 1997/7/8
Y1 - 1997/7/8
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0030761589&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(97)00294-1
DO - 10.1016/S0960-894X(97)00294-1
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AN - SCOPUS:0030761589
SN - 0960-894X
VL - 7
SP - 1709
EP - 1714
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 13
ER -