Synthesis and biological evaluation of a new series of phenothiazine- containing protein farnesyltransferase inhibitors

Article abstract of DOI:10.1016/j.ejmech.2012.11.008

Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC₅₀ values of 0.7 and 0.6 μM, respectively.