Abstract
A series of novel podophyllotoxin derivatives was synthesized by coupling 4β-amino-4′-demethyl-4-desoxypodophyllotoxin (3a) or 4β-amino-4-desoxypodophyllotoxin (3b) with N-substituted 5-formylindole (2a–h). Their structures were identied by spectroscopic techniques. These novel derivatives were evaluated for cytotoxicity in vitro against HepG2 and HeLa cell lines. Compared with etoposide, most of the compounds showed more potent cytotoxicities against two tumor cell lines. Judging from the IC50 values, compound 5n is a promising agent, which is about 15 and 5 times more toxic than etoposide against HepG2 and HeLa cell lines, respectively.
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