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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Dumitriu GM,Ghinet A,Bîcu E,Rigo B,Dubois J,Farce A,Belei Ddoi
10.1016/j.bmcl.2014.04.102subject
Has Abstractpub_date
2014-07-15 00:00:00pages
3180-5issue
14eissn
0960-894Xissn
1464-3405pii
S0960-894X(14)00459-4journal_volume
24pub_type
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