New analogue of arenastatin A, a potent cytotoxic spongean depsipeptide, with anti-tumor activity |
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Authors: | Murakami Nobutoshi Tamura Satoru Koyama Kouhei Sugimoto Masanori Maekawa Ryuji Kobayashi Motomasa |
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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: | Two analogues possessing steric hindered substituents on C-15 of arenastatin A (1), a potent cytotoxic spongean depsipeptide, were synthesized and shown to enhance stability in mouse serum. Notably, 15-tert-butylanalogue (6) with higher cytotoxicity exhibited in vivo anti-tumor activity through iv administration different from 1. Additionally, conformation analysis among the two analogues and arenastatin A (1) indicated that the torsion angle from C-14 to C-20 is a conclusive factor for the potent cytotoxicity of 1. |
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