Structures and cytotoxicity relationship of isoaaptamine and aaptamine derivatives

A series of 9-O-acylisoaaptamine (3-14) and 4-N-acyl-dihydroaaptamine (16-1 9) derivatives have been prepared and evaluated for antitumor activity agai nst murine P-388 and human tumor cells including KB16, A549, and HT-29 cell lines. All of compounds showed significant cytotoxicity against P-388 cell s. Among them, compounds 9-11 showed potent activity as isoaaptamine (1). T here was an apparent lack of linear relationship between cytotoxicity and c arbon number of the side chain. The structure and activity relationship for these particular compounds are discussed.