Synthesis of aristolactam analogues and evaluation of their antitumor activity |
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Authors: | Young Lok Choi Joa Kyum Kim Sang-Un Choi Yong-Ki Min Myung-Ae Bae Bum Tae Kim Jung-Nyoung Heo |
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Affiliation: | 1. Bioorganic Science Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea;2. Department of Chemistry, Sungkyunkwan University, Suwon 440-746, Republic of Korea |
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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 GI50 values in the submicromolar range. |
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