Title of article
Paclitaxel esters of malic acid as prodrugs with improved water solubility Original Research Article
Author/Authors
Eric W.P Damen، نويسنده , , Peter H.G Wiegerinck، نويسنده , , Lesly Braamer، نويسنده , , Duncan Sperling، نويسنده , , Dick de Vos، نويسنده , , Hans W. Scheeren، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
6
From page
427
To page
432
Abstract
The synthesis of paclitaxel esters of malic acid is described. These compounds were found to have improved water solubility and are stable in solution at neutral pH. The C2′ modified compounds behave as prodrugs, that is, paclitaxel is generated upon exposure to human plasma, whereas the C7 modified derivatives do not. 2′-Malyl paclitaxel sodium salt demonstrated enhanced antitumour activity and less toxicity in a P388 murine leukaemia in vivo model when compared to paclitaxel.
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2000
Journal title
Bioorganic and Medicinal Chemistry
Record number
1300854
Link To Document