7-imidazolylalkanamido-1-carboxylalkylbenzo-diazepine, a novel series of farnesyltransferase inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 516-521, 2002.
Article
in English
| WPRIM
| ID: wpr-251110
ABSTRACT
<p><b>AIM</b>Design, synthesis and evaluation of a series of 7-imidazolylalkanamido-1-carboxylalkylbenzodiazepine farnesyltransferase (FTase) inhibitors.</p><p><b>METHODS AND RESULTS</b>Coupling 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.</p><p><b>CONCLUSION</b>Five target compounds were found to be potential farnesyltransferase inhibitors.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Benzodiazepines
/
Molecular Structure
/
Chemistry
/
Alkyl and Aryl Transferases
/
Inhibitory Concentration 50
/
Farnesyltranstransferase
/
Imidazoles
/
Molecular Conformation
Language:
English
Journal:
Acta Pharmaceutica Sinica
Year:
2002
Type:
Article
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