Document Detail


Piperazimycins: cytotoxic hexadepsipeptides from a marine-derived bacterium of the genus Streptomyces.
MedLine Citation:
PMID:  17221946     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Three potent cancer cell cytotoxins, piperazimycins A-C (1-3), have been isolated from the fermentation broth of a Streptomyces sp., cultivated from marine sediments near the island of Guam. The structures of these cyclic hexadepsipeptides were assigned by a combination of spectral, chemical, and crystallographic methods. The piperazimycins are composed of rare amino acids, including hydroxyacetic acid, alpha-methylserine, gamma-hydroxypiperazic acid, and gamma-chloropiperazic acid. The novel amino acid residues 2-amino-8-methyl-4,6-nonadienoic acid and 2-amino-8-methyl-4,6-decadienoic acid were found as components of piperazimycins A and C, respectively. When screened in the National Cancer Institute's 60 cancer cell line panel, piperazimycin A exhibited potent in vitro cytotoxicity toward multiple tumor cell lines with a mean GI50 of 100 nM.
Authors:
Eric D Miller; Christopher A Kauffman; Paul R Jensen; William Fenical
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  The Journal of organic chemistry     Volume:  72     ISSN:  0022-3263     ISO Abbreviation:  J. Org. Chem.     Publication Date:  2007 Jan 
Date Detail:
Created Date:  2007-01-15     Completed Date:  2007-03-20     Revised Date:  2007-12-03    
Medline Journal Info:
Nlm Unique ID:  2985193R     Medline TA:  J Org Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  323-30     Citation Subset:  IM    
Affiliation:
Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California-San Diego, La Jolla, California 92093-0204, USA.
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MeSH Terms
Descriptor/Qualifier:
Cell Line, Tumor
Cell Proliferation / drug effects
Crystallography, X-Ray
Depsipeptides / chemistry,  isolation & purification,  pharmacology*
Drug Screening Assays, Antitumor
Humans
Magnetic Resonance Spectroscopy / methods,  standards
Models, Molecular
Molecular Conformation
Reference Standards
Sensitivity and Specificity
Stereoisomerism
Streptomyces / chemistry*
Structure-Activity Relationship
Grant Support
ID/Acronym/Agency:
CA44848/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Depsipeptides; 0/piperazimycin A; 0/piperazimycin B; 0/piperazimycin C

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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