期刊
CHEMISTRY-AN ASIAN JOURNAL
卷 7, 期 7, 页码 1616-1623出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.201101049
关键词
cancer; inhibitor; lamellarin; multidrug resistance; p-glycoprotein
资金
- Institute for Molecular Bioscience
- University of Queensland
- Australian Research Council (ARC) [LP0775547]
- Noscira (Madrid, Spain)
- Australian Research Council [LP0775547] Funding Source: Australian Research Council
Chemical analysis of a Didemnum sp. (CMB-01656) collected during scientific Scuba operations off Wasp Island, New South Wales, yielded five new lamellarins A1 (1), A2 (2), A3 (3), A4 (4) and A5 (5) and eight known lamellarins C (6), E (7), K (8), M (9), S (10), T (11), X (12) and ? (13). Analysis of a second Didemnum sp. (CMB-02127) collected during scientific trawling operations along the Northern Rottnest Shelf, Western Australia, yielded the new lamellarin A6 (14) and two known lamellarins G (15) and Z (16). Structures were assigned to 116 on the basis of detailed spectroscopic analysis with comparison to literature data and authentic samples. Access to this unique library of natural lamellarins (116) provided a rare opportunity for structureactivity relationship (SAR) investigations, probing interactions between lamellarins and the ABC transporter efflux pump P-glycoprotein (P-gp) with a view to reversing multidrug resistance in a human colon cancer cell line (SW620 Ad300). These SAR studies, which were expanded to include the permethylated lamellarin derivative (17) and a series of lamellarin-inspired synthetic coumarins (1924) and isoquinolines (2526), successfully revealed 17 as a promising new non-cytotoxic P-gp inhibitor pharmacophore.
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