7-imidazolylalkanamido-1-carboxylalkylbenzo-diazepine, a novel series of farnesyltransferase inhibitors.
OBJECTIVE
Design, synthesis and evaluation of a series of 7-imidazolylalkanamido-1-carboxylalkylbenzodiazepine farnesyltransferase (FTase) inhibitors.


RESULTS
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.


CONCLUSIONS
Five target compounds were found to be potential farnesyltransferase inhibitors.
Wan
Sheng-biao
SB
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
Chu
Feng-ming
FM
Guo
Zong-ru
ZR
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors* / Q000187:drug effects; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D051231:Farnesyltranstransferase; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008968:Molecular Conformation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D007093:Imidazoles; D001569:Benzodiazepines; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase