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Eur J Med Chem. 2003 Oct;38(10):899-911.

Synthesis, cytotoxicity and antiviral activity of podophyllotoxin analogues modified in the E-ring.

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Departamento de Química Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, 37007 Salamanca, Spain.


Several podophyllotoxin derivatives modified in the E-ring were prepared and evaluated for their cytotoxicity on four neoplastic cell lines (P-388, A-549, HT-29 and MEL-28) and for their antiherpetic activity against Herpes simplex virus type II. The trimethoxyphenyl moiety was oxidized to ortho-quinone and further condensed with diamines and enamines to form different heterocycles. Most of the compounds maintained their cytotoxicity at the muM level and some of them showed antiherpetic activity.

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