Synthesis and biological activities of reveromycin A and spirofungin A derivatives |
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| Authors: | Shimizu Takeshi Usui Takeo Fujikura Makoto Kawatani Makoto Satoh Tomoharu Machida Kiyotaka Kanoh Naoki Woo Je-Tae Osada Hiroyuki Sodeoka Mikiko |
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| Affiliation: | Synthetic Organic Chemistry Laboratory, RIKEN (The Institute of Physical and Chemical Research), Wako, Saitama 351-0198, Japan. tshimizu@riken.jp |
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| Abstract: | Various derivatives of reveromycin A, an inhibitor of eukaryotic cell growth, and spirofungin A, focusing on the 5S hydroxyl group and C18 hemisuccinyl group, were synthesized and their inhibitory effects on both the isoleucyl-tRNA synthetase activity and the survival of osteoclasts, and activities on the morphological reversion of src(ts)-NRK cells were examined. It was found that 2,3-dihydroreveromycin A is the promising derivative of reveromycin A based on the activity and stability. |
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