2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Williams
T M
TM
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA.
Ciccarone
T M
TM
MacTough
S C
SC
Bock
R L
RL
Conner
M W
MW
Davide
J P
JP
Hamilton
K
K
Koblan
K S
KS
Kohl
N E
NE
Kral
A M
AM
Mosser
S D
SD
Omer
C A
CA
Pompliano
D L
DL
Rands
E
E
Schaber
M D
MD
Shah
D
D
Wilson
F R
FR
Gibbs
J B
JB
Graham
S L
SL
Hartman
G D
GD
Oliff
A I
AI
Smith
R L
RL
D019883:Alkyl and Aryl Transferases; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016923:Cell Death / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D002461:Cell Line, Transformed; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051231:Farnesyltranstransferase; D051379:Mice; D008819:Mice, Nude; D008968:Molecular Conformation; D015394:Molecular Structure; D009368:Neoplasm Transplantation; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011106:Polyisoprenyl Phosphates / Q000378:metabolism; D017368:Protein Prenylation; D011499:Protein Processing, Post-Translational / Q000187:drug effects; D051381:Rats; D012513:Sarcoma, Experimental / Q000188:drug therapy / Q000473:pathology; D012717:Sesquiterpenes; D014166:Transferases / Q000037:antagonists & inhibitors*; D018631:ras Proteins / Q000378:metabolism
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D010879:Piperazines; D011106:Polyisoprenyl Phosphates; D012717:Sesquiterpenes; C004808:farnesyl pyrophosphate; D014166:Transferases; D019883:Alkyl and Aryl Transferases; C083291:geranylgeranyltransferase type-I; D051231:Farnesyltranstransferase; D018631:ras Proteins