1.
Bioorg Med Chem Lett
; 15(24): 5407-11, 2005 Dec 15.
Article
in English
| MEDLINE
| ID: mdl-16216509
ABSTRACT
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.
Subject(s)
Enzyme Inhibitors/chemical synthesis , Farnesyltranstransferase/antagonists & inhibitors , Triazoles/chemical synthesis , Amino Acid Sequence , Enzyme Inhibitors/pharmacology , Farnesyltranstransferase/genetics , Genes, ras , Models, Molecular , Molecular Conformation , Oligopeptides/chemistry , Triazoles/pharmacology
2.
Bioorg Med Chem Lett
; 13(9): 1543-7, 2003 May 05.
Article
in English
| MEDLINE
| ID: mdl-12699751
ABSTRACT
The evaluation of structure-activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.
