Structures and cytotoxicity relationship of isoaaptamine and aaptamine derivatives.
A series of 9-O-acylisoaaptamine (3-14) and 4-N-acyl-dihydroaaptamine (16-19) derivatives have been prepared and evaluated for antitumor activity against murine P-388 and human tumor cells including KB16, A549, and HT-29 cell lines. All of compounds showed significant cytotoxicity against P-388 cells. Among them, compounds 9-11 showed potent activity as isoaaptamine (1). There was an apparent lack of linear relationship between cytotoxicity and carbon number of the side chain. The structure and activity relationship for these particular compounds are discussed.
Shen
Y C
YC
Institute of Marine Resources, National Sun Yat-sen University, 70 Lien-Hai Road, Kaohsiung, Taiwan, Republic of China. ycshen@mail.nsysu.edu.tw
Lin
T T
TT
Sheu
J H
JH
Duh
C Y
CY
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D009287:Naphthyridines / Q000737:chemistry* / Q000494:pharmacology*; D011161:Porifera / Q000737:chemistry; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D009287:Naphthyridines; C043986:aaptamine