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3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors

โœ Scribed by Charles Z Ding; John T Hunt; Carol Ricca; Veeraswamy Manne


Book ID
104364968
Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
108 KB
Volume
10
Category
Article
ISSN
0960-894X

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โœฆ Synopsis


Design, synthesis and structure-activity relationship of a series of 3-imidazolylmethylaminophenylsulfonyltetrahydroquinolines as farnesyltransferase inhibitors are presented. A working pharmacophore of inhibiting farnesyltransferase by this series of inhibitors is proposed.


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## Abstract The development of farnesyltransferase inhibitors directed against __Plasmodium falciparum__ is a strategy towards new drugs against malaria. Previously, we described benzophenoneโ€based farnesyltransferase inhibitors with high inโ€…vitro antimalarial activity but no inโ€…vivo activity. Thro