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Design, Synthesis, and Evaluation of Novel Modular Bisubstrate Analogue Inhibitors of Farnesyltransferase
Author(s) -
Schlitzer Martin,
Sattler Isabel
Publication year - 1999
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/(sici)1521-3773(19990712)38:13/14<2032::aid-anie2032>3.0.co;2-d
Subject(s) - farnesyltransferase , farnesyltransferase inhibitor , modular design , farnesyl diphosphate farnesyltransferase , chemistry , combinatorial chemistry , pharmacology , enzyme , computer science , biochemistry , medicine , prenylation , operating system
Promising potential chemotherapeutics for the treatment of cancer can be developed from farnesyltransferase inhibitors. A novel class of modular bisubstrate farnesyltransferase inhibitors is presented that can be synthesized in a straightforward manner. An example of such an inhibitor is compound 1 , which has an IC 50 value of 3.7 μ M .