Synthesis of aristolactam analogues and evaluation of their antitumor activity.
A series of natural aristolactams and their analogues have been prepared and evaluated for antitumor activity against human cancer cells, including multi-drug resistant cell lines. Naturally occurring aristolactams, such as aristolactam BII (cepharanone B), aristolactam BIII, aristolactam FI (piperolactam A), N-methyl piperolactam A, and sauristolactam showed moderate antitumor activities in selected cell lines. However, several synthetic aristolactam derivatives exhibited potent antitumor activities against a broad array of cancer cell lines with GI(50) values in the submicromolar range.
Choi
Young Lok
YL
Bioorganic Science Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
Kim
Joa Kyum
JK
Choi
Sang-Un
SU
Min
Yong-Ki
YK
Bae
Myung-Ae
MA
Kim
Bum Tae
BT
Heo
Jung-Nyoung
JN
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001060:Aporphines / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D007769:Lactams / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity
D000970:Antineoplastic Agents; D001060:Aporphines; D006576:Heterocyclic Compounds, 4 or More Rings; D007769:Lactams; C081279:aporphine