302969-60-4Relevant articles and documents
Non-thiol farnesyltransferase inhibitors: The concept of benzophenone- based bisubstrate analogue farnesyltransferase inhibitors
Schlitzer, Martin,Sattler, Isabel
, p. 721 - 726 (2000)
Replacement of the thiol in a benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitor by a carboxylic acid moiety resulted in a marked drop in inhibitory potency. Transformation of these carboxylic acid derivatives into bisubstrate analogues by addition of a lipophilic alkyl chain, which should be able to occupy considerable portions of the farnesyl binding region in the farnesyltransferase's active site, resulted in a regain of the inhibitory activity. The bisubstrate analogues represent new lead structures for non-thiol farnesyltransferase inhibitors. (C) 2000 Editions scientifiques et medicales Elsevier SAS.