Synthesis, cytotoxicity, metabolic stability and pharmacokinetic evaluation of fluorinated docetaxel analogs

Three novel fluorinated docetaxel analogs, along with six previous reported, were evaluated for their cytotoxicity against five tumor cell lines. The results indicated that these analogs maintained similar/more potent activity than docetaxel against these tumor cell lines. They were also evaluated for their metabolic stability and pharmacokinetics, which demonstrated that these analogs showed better profiles of metabolic stability and pharmacokinetics than that of docetaxel.

Three novel fluorinated docetaxel analogs, along with six previous reported, were evaluated for their cytotoxicity, metabolic stability and pharmacokinetics, which demonstrated that these analogs showed better profiles than docetaxel.Figure optionsDownload as PowerPoint slideHighlights
► Three novel fluorinated docetaxel analogs were synthesized.
►  These analogs maintained similar/more potent cytotoxicity than docetaxel.
► These analogs also showed better profiles of metabolic stability and pharmacokinetics.