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Bioorg Med Chem. 2004 Jun 15;12(12):3339-44.

Antitumor agents. Part 227: Studies on novel 4'-O-demethyl-epipodophyllotoxins as antitumor agents targeting topoisomerase II.

Author information

1
Natural Products Laboratory, School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599-7360, USA.

Abstract

Eight novel epipodophyllotoxin derivatives (6-13), which were designed to overcome drug resistance and enhance topoisomerase II inhibition, were synthesized and evaluated. Two of these compounds (7 and 8) showed better preclinical activity profiles, including cell growth inhibition, cell killing, and in vitro topoisomerase II inhibition, as compared to the prototype molecule etoposide (1). They also retained the superior drug-resistance profile of GL-331 (4), an epipodophyllotoxin derivative currently in clinical evaluation.

PMID:
15158802
DOI:
10.1016/j.bmc.2004.03.067
[Indexed for MEDLINE]

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