2. Academic Validation
  3. Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid

Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid

  • Bioorg Med Chem. 2007 Sep 15;15(18):6323-30. doi: 10.1016/j.bmc.2007.04.002.
Wenting Du 1,  Lan Hong,  Tongwei Yao,  Xiaochun Yang,  Qiaojun He,  Bo Yang,  Yongzhou Hu
Affiliations

Affiliation

  • 1 ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
PMID: 17624790 DOI: 10.1016/j.bmc.2007.04.002
Abstract

The synthesis of docetaxel esters of malic acid is described. These compounds were found to have greatly improved water solubility and are stable in solution at neutral pH. The C2' modified compounds 2a-c and 3a-c behave as prodrugs, that is, docetaxel is generated upon exposure to human plasma, whereas the C7 and C2',7,10- l modified derivatives do not. 2'-dl-Malyl docetaxel sodium salt demonstrated enhanced antitumor activity in vitro when compared to docetaxel and showed the inhibitory effect on tumor growth in vivo.

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