Synthesis and Evaluation of Water-Soluble Etoposide Esters of Malic Acid as Prodrugs

Author(s): Jing Chen, Wenting Du.

Journal Name: Medicinal Chemistry

Volume 9 , Issue 5 , 2013

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Abstract:

Thirty etopside esters of malic acid were synthesized and have been shown to exhibit improved aqueous solubility and stability in neutral solution except for compounds 7Ia-c and 9Ia-c. Compounds 6Ia–c, 6IIb-c, 8Ia-b and 10Ib have been shown to function as prodrugs, whereas the other synthesized derivatives were too stable to reveal parent drugs in vivo. Among synthesized compounds, 8Ib, 4’-O-demethyl 4’-L-malyl epipodophyllotoxins showed the most potent anticancer activity and favorable stability in vitro.

Keywords: Anticancer, Etoposide, Malic Acid, Prodrugs, Synthesis, Water-Soluble.

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Article Details

VOLUME: 9
ISSUE: 5
Year: 2013
Page: [740 - 747]
Pages: 8
DOI: 10.2174/1573406411309050014
Price: $58

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