Synthesis of 15,20-triamide analogue with polar substituent on the phenyl ring of arenastatin A, an extremely potent cytotoxic spongean depsipeptide |
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Authors: | Kotoku Naoyuki Kato Tomoya Narumi Fuminori Ohtani Emiko Kamada Sayo Aoki Shunji Okada Naoki Nakagawa Shinsaku Kobayashi Motomasa |
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Institution: | Department of Natural Product Chemistry, Graduate School of Pharmaceutical Sciences, Osaka University, Japan. |
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Abstract: | In order to increase metabolic stability and water solubility of arenastatin A, an extremely potent cytotoxic depsipeptide from the Okinawan marine sponge of Dysidea arenaria, several 15,20-triamide analogues with a polar substituent on the phenyl ring were synthesized. The 15,20-triamide analogues with a polar substituent (24, 30, and 31) showed increased solubility to MeOH and stronger cytotoxicity against KB cells in comparison with the parental 15,20-triamide analogue (2). Furthermore, the diethylamine analogue (30) exhibited in vivo anti-tumor activity against subcutaneously implanted murine sarcoma. |
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