The antiproliferative effect of acridone alkaloids on several cancer cell lines.
Fifteen acridone alkaloids were examined for their antiproliferative activity toward monolayers and suspension of several types of cancer and normal human cell lines. As a result, atalaphyllidine (9), 5-hydroxy-N-methylseverifoline (11), atalaphyllinine (12), and des-N-methylnoracronycine (13) showed potent antiproliferative activity against tumor cell lines, whereas they have weak cytotoxicity on normal human cell lines. The structure-activity relationship established from the results revealed that a secondary amine, hydroxyl groups at C-1 and C-5, and a prenyl group at C-2 played an important role for antiproliferative activities of the tetracyclic acridones.
Kawaii
S
S
National Institute of Fruit Tree Science, Okitsu, Shimizu, Shizuoka, 424-0204, Japan.
Tomono
Y
Y
Katase
E
E
Ogawa
K
K
Yano
M
M
Takemura
Y
Y
Ju-ichi
M
M
Ito
C
C
Furukawa
H
H
D000166:Acridines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D054831:Acridones; D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000166:Acridines; D054831:Acridones; D000470:Alkaloids; D000970:Antineoplastic Agents; C041300:acridone