Novel triazole based inhibitors of Ras farnesyl transferase.
A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC(50) value of less than 1nM.
Saha
Ashis K
AK
Department of Medicinal Chemistry, Janssen Research Foundation, Johnson & Johnson Pharmaceutical Research & Development, Welsh and McKean Roads, Spring House, PA 19477, USA. asaha@predixpharm.com
Liu
Li
L
Simoneaux
Richard
R
DeCorte
Bart
B
Meyer
Christophe
C
Skrzat
Stacy
S
Breslin
Henry J
HJ
Kukla
Michael J
MJ
End
Dave W
DW
D000595:Amino Acid Sequence; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors* / Q000235:genetics; D011905:Genes, ras; D008958:Models, Molecular; D008968:Molecular Conformation; D009842:Oligopeptides / Q000737:chemistry; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D004791:Enzyme Inhibitors; D009842:Oligopeptides; D014230:Triazoles; D051231:Farnesyltranstransferase