- Synthesis of stable analogs in blood and conformational analysis of arenastatin A, a potent cytotoxic spongean depsipeptide
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In order to produce stable analogs in blood of arenastatin A, a potent cytotoxic depsipeptide from the marine sponge Dysidea arenaria, we synthesized four analogs in which the 15-20 ester linkage was modified. Among them, the carba analog and 20-deoxo analog showed stability in serum. The conformation of arenastatin A and its three analogs were analyzed by distance-restrained molecular dynamic calculation to elucidate a three-dimensional stereostructure contributing to the extremely potent cytotoxicity of arenastatin A.
- Murakami, Nobutoshi,Tamura, Satoru,Wang, Weiqi,Takagi, Tatsuya,Kobayashi, Motomasa
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p. 4323 - 4336
(2007/10/03)
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- Synthesis and biological property of carba and 20-deoxo analogues of arenastatin A
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The carba analogue, in which a methylene group is substituted for the oxygen atom linked to C-15, and 20-deoxo analogue of arenastatin A, a potent cytotoxic spongean depsipeptide, were synthesized. Both analogues lacking the 15,20-ester function, which was easily metabolized in serum, showed good stability in serum as well as moderate cytotoxic activity against KB cells and better solubility. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Murakami, Nobutoshi,Wang, Weiqi,Tamura, Satoru,Kobayashi, Motomasa
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p. 1823 - 1826
(2007/10/03)
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