Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues

HF Lu, X Sun, L Xu, LG Lou, GQ Lin

Index: Lu, Hong-Fu; Sun, Xun; Xu, Liang; Lou, Li-Guang; Lin, Guo-Qiang European Journal of Medicinal Chemistry, 2009 , vol. 44, # 2 p. 482 - 491

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Citation Number: 13

Abstract

A series of novel fluorinated docetaxel analogues have been synthesized and evaluated in vitro and in vivo. Incorporated one, two or three fluorine atom (s) either at both meta position on C-2 benzolate and 3′-N-tert-butyloxyl group or only at 3′-N-tert-butyloxyl group has resulted in potent analogues which have comparable or superior in vitro and in vivo cytotoxicity to docetaxel. Among them, compounds 14d and 14e have displayed more ...