| Literature DB >> 17624790 |
Wenting Du1, Lan Hong, Tongwei Yao, Xiaochun Yang, Qiaojun He, Bo Yang, Yongzhou Hu.
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.Entities:
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Year: 2007 PMID： 17624790 DOI： 10.1016/j.bmc.2007.04.002
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641