Concise synthesis and structure-activity relationship of furospinosulin-1, a hypoxia-selective growth inhibitor from marine sponge |
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Authors: | Naoyuki Kotoku Shinichi FujiokaChiaki Nakata Masaki YamadaYuji Sumii Takashi KawachiMasayoshi Arai Motomasa Kobayashi |
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Institution: | Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan |
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Abstract: | Structure-activity relationship of furospinosulin-1 (1), a hypoxia-selective growth inhibitor isolated from marine sponge, was investigated. Concise synthetic method of 1 was developed, and some structurally modified analogues were prepared. Biological evaluation of them revealed that the whole chemical structure was important for the hypoxia-selective growth inhibitory activity of 1. Among prepared, the desmethyl analogue 30 showed excellent hypoxia-selective inhibitory activity similar to that of 1 and also exhibited in vivo anti-tumor activity with oral administration. |
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Keywords: | Furospinosulin-1 Hypoxia-selective growth inhibitor Marine sponge Analogue compound |
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