期刊
TETRAHEDRON LETTERS
卷 51, 期 51, 页码 6718-6721出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2010.10.062
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资金
- Alzheimer's Association [NIRG-08-90880]
- Alzheimer's Drug Discovery Foundation [281204]
- National Institute of Aging [R20072671]
- National Science Foundation [CHE9974921]
- Elsa Pardee Foundation
- Department of Defense [W911NF-04-1-0344]
- NIH MBRS SCORE [S06-GM-44796]
Bouillomides A (1) and B (2) are two depsipeptide analogues of dolastatin 13. Isolated from a Guamanian sample of Lyngbya bouillonii, the planar structures were elucidated on the basis of HR-ESI-MS and NMR data, while the absolute configurations were determined by employing functional group conversions, modified Marfey's analysis, and detailed analyses of ROESY correlations. Compounds 1 and 2 selectively inhibited serine proteases elastase (IC50=1.9 mu M for both) and chymotrypsin (IC50 = 0.17 and 9.3 mu M, respectively) while showing no inhibition of trypsin (IC50 > 100 mu M). (C) 2010 Elsevier Ltd. All rights reserved.
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