New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation.
Basic Information
ID: ALA3826975
Journal: Bioorg Med Chem Lett
Title: New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation.
Authors: Moise IM, Ghinet A, Belei D, Dubois J, Farce A, Bîcu E.
Abstract: A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine 2a, exhibiting an IC50 value in the low nanomolar range, similar to that of known FTI-276, highly potent farnesyltransferase inhibitor. The newly synthesized indolizine-chalcones 2a-d constitute the most efficient inhibitors of farnesyltransferase bearing a phenothiazine unit known to date.
CiteXplore: 27282741
DOI: 10.1016/j.bmcl.2016.05.074
Patent ID: ┄