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Synthesis of aristolactam analogues and evaluation of their antitumor activity
Young Lok Choi1, Joa Kyum Kim, Sang-Un Choi
1Bioorganic Science Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
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.
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