Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogues of the potent FTI, 4-[3-biphenyl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile, were synthesized and tested in vitro for their inhibitory activities. The synthesis and detailed biological data of this series of analogues are presented.
Lin
Nan-Horng
NH
Cancer Research, D-47B, Global Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. nanhorng.lin@abbott.com
Wang
Le
L
Cohen
Jerry
J
Gu
Wen-Zhen
WZ
Frost
David
D
Zhang
Haiying
H
Rosenberg
Saul
S
Sham
Hing
H
D016475:3T3 Cells; D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D051231:Farnesyltranstransferase; D011905:Genes, ras / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D009570:Nitriles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D005723:gamma-Glutamyltransferase / Q000037:antagonists & inhibitors
C478322:4-(3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl)-1-yl-benzonitrile; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007093:Imidazoles; D009570:Nitriles; D005723:gamma-Glutamyltransferase; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase