Abstract：
:Borrelidin A (1) is produced by several species of Streptomyces and within its bioactive scaffold, the vinylic nitrile moiety is essential for activity. We report herein newly discovered members of the borrelidin family, borrelidin F (2), borrelidin G (3), borrelidin H (4) and borrelidin I (5); all were isolated from Streptomyces rochei SCSIO ZJ89 originating from a mangrove-derived sediment sample. These structurally diverse metabolites enabled a number of new structure-activity relationships (SARs) to be identified, especially with respect to the different configurations at the C11-OH and C12-C15 double bonds for which the absolute configurations were determined using spectroscopic methods. Importantly, borrelidin H (4) was found to have a therapeutic window superior to that of borrelidin A (1) in vitro and could inhibit migration of cancer cells.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Sun J,Shao J,Sun C,Song Y,Li Q,Lu L,Hu Y,Gui C,Zhang H,Ju Jdoi
10.1016/j.bmc.2018.01.010subject
Has Abstractpub_date
2018-05-01 00:00:00pages
1488-1494issue
8eissn
0968-0896issn
1464-3391pii
S0968-0896(17)32332-5journal_volume
26pub_type
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