Synthesis and cytotoxicity of 2alpha-amido docetaxel analogues

  • Bioorg Med Chem Lett. 2002 Jun 3;12(11):1543-6. doi: 10.1016/s0960-894x(02)00118-x.
Wei-Shuo Fang  1 ,  Ying Liu ,  Hong-Yan Liu ,  Shao-Feng Xu ,  Liang Wang ,  Qi-Cheng Fang
Affiliations
  • 1. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, PR China. [email protected]
PMID: 12031338 DOI: 10.1016/s0960-894x(02)00118-x
Abstract

Various 2-amido docetaxel analogues were prepared and evaluated for their cytotoxicities. Among them, m-methoxy and m-chlorobenzoylamido analogues were most active but not superior to docetaxel and paclitaxel, and D-seco analogues inactive. Change of 2-benzoate to 2-benzamide may not improve their activities to drug-resistant cell lines.