4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 5, Pages 1743-1748

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.02.027

Keywords

Fluorinated docetaxel analogs; Cytotoxicity; Metabolic stability; Pharmacokinetics

Funding

  1. National Natural Science Foundation of China [20772017]
  2. National Drug Innovative Program [2009ZX09301-011]
  3. Shanghai Municipal Committee of Science and Technology [07DZ19713]

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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. Crown Copyright (C) 2011 Published by Elsevier Masson SAS. All rights reserved.

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