Abstract
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.
Original language | English |
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Pages (from-to) | 4323-4336 |
Number of pages | 14 |
Journal | Tetrahedron |
Volume | 57 |
Issue number | 20 |
DOIs | |
Publication status | Published - 2001 May 14 |
Keywords
- Arenastatin A
- Depsipeptide
- Marine metabolite
- Restrained molecular dynamics
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry