Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors
ABSTRACT A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice.
SourceAvailable from: Guri L.V.Damu
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ABSTRACT: Novel phenothiazine derivatives bearing an amino acid residue were synthesized via peptide chemistry, and evaluated for their inhibitory potential on human farnesyltransferase. The phenothiazine unit proved to be an important bulky unit in the structure of the synthesized inhibitors. Propargyl ester 20 bearing a tyrosine residue exhibited the best biological potential in vitro in the present study. Further syntheses and biological evaluation of phenothiazine derivatives are necessary in order to gain a full view of SAR in this family of farnesyltransferase inhibitors.Bioorganic & Medicinal Chemistry Letters 05/2014; DOI:10.1016/j.bmcl.2014.04.102 · 2.33 Impact Factor
European Journal of Medicinal Chemistry 11/2014; · 3.43 Impact Factor