title: Synthesis of aristolactam analogues and evaluation of their antitumor activity.
abstract: 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.
authors.affiliation: Bioorganic Science Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
authors.forename: Young Lok
authors.initials: YL
authors.lastname: Choi
authors.forename: Joa Kyum
authors.initials: JK
authors.lastname: Kim
authors.forename: Sang-Un
authors.initials: SU
authors.lastname: Choi
authors.forename: Yong-Ki
authors.initials: YK
authors.lastname: Min
authors.forename: Myung-Ae
authors.initials: MA
authors.lastname: Bae
authors.forename: Bum Tae
authors.initials: BT
authors.lastname: Kim
authors.forename: Jung-Nyoung
authors.initials: JN
authors.lastname: Heo
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D001060:Aporphines; D006576:Heterocyclic Compounds, 4 or More Rings; D007769:Lactams; C081279:aporphine