Abstract
4-Aza-2,3-dehydro-4-deoxypodophyllotoxin analogues 3a–n were synthesized through quinolines 2a–n. Comparison of their cytotoxicity against P-388 leukemia cells revealed that the steric effects of the ring B substituents on the activity are greater than the electronic effects, while the presence of a methoxy group on the ring E is not essential to exhibit potent cytotoxicity. Analogues 3a and 3b proved to be more than twice as cytotoxic as natural podophyllotoxin (1).
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