Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368549 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Iuliana-Monica Moise, Alina Ghinet, Dalila Belei, Joëlle Dubois, Amaury Farce, Elena Bîcu,