7-imidazolylalkanamido-1-carboxylalkylbenzo-diazepine, a novel series of farnesyltransferase inhibitors.
- Author:
Sheng-biao WAN
1
;
Feng-ming CHU
;
Zong-ru GUO
Author Information
- Publication Type:Journal Article
- MeSH: Alkyl and Aryl Transferases; antagonists & inhibitors; drug effects; Benzodiazepines; chemical synthesis; chemistry; pharmacology; Farnesyltranstransferase; Imidazoles; chemical synthesis; chemistry; pharmacology; Inhibitory Concentration 50; Molecular Conformation; Molecular Structure; Structure-Activity Relationship
- From: Acta Pharmaceutica Sinica 2002;37(7):516-521
- CountryChina
- Language:English
-
Abstract:
AIMDesign, synthesis and evaluation of a series of 7-imidazolylalkanamido-1-carboxylalkylbenzodiazepine farnesyltransferase (FTase) inhibitors.
METHODS AND RESULTSCoupling of imidazolylalkylcarboxylic acids and 1-substituted 7-aminobenzodiazepines (5a-5c) yielded 10 new compounds (6-12, 16-18) which were biologically tested against FTase using scintillation proximity assay method.
CONCLUSIONFive target compounds were found to be potential farnesyltransferase inhibitors.
