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7-imidazolylalkanamido-1-carboxylalkylbenzo-diazepine, a novel series of farnesyltransferase inhibitors.

作者信息

Wan Sheng-biao, Chu Feng-ming, Guo Zong-ru

机构信息

Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.

出版信息

Yao Xue Xue Bao. 2002 Jul;37(7):516-21.

Abstract

AIM

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

METHODS AND 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.

CONCLUSION

Five target compounds were found to be potential farnesyltransferase inhibitors.

摘要

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