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

Jing      Chen; Wenting      Du

doi:10.2174/1573406411309050014

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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Medicinal Chemistry

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

Volume: 9 Issue: 5

Author(s): Jing Chen and Wenting Du

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

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.

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Chen Jing and Du Wenting, Synthesis and Evaluation of Water-Soluble Etoposide Esters of Malic Acid as Prodrugs, Medicinal Chemistry 2013; 9 (5) . https://dx.doi.org/10.2174/1573406411309050014