期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 17, 期 4, 页码 1319-1326出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201001547
关键词
aspergiolides; isotopic labeling; natural products; polyketides; quantum chemical calculations; receptors
资金
- Chinese National Science Fund [30973627, 30672527]
- National High Technology Research and Development Program of China [2006AA09Z429]
- State Key Laboratory of Drug Research Fund [SIMM0901KF-05]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT0944]
- Deutsche Forschungsgemeinschaft [SFB 630]
- Natural Science Foundation of China for Distinguished Young Scholars [30725046]
- State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Variation of the cultivation conditions for Aspergillus glaucus led to the discovery of two novel spirocyclic aromatic polyketides, aspergiolides C (3) and D (4). Their constitutions were elucidated by a combination of spectroscopic methods and isotope-labeling experiments. Aspergiolides C (3) and D (4) occur as racemic mixtures, the resolution of which was succeeded by HPLC on a chiral phase. The absolute configurations of their enantiomers were assigned online, from the peaks in the chromatogram, by a combination of HPLC-CD and quantum chemical CD calculations. Both compounds were found to inhibit the kinase activities of the receptor tyrosine kinases (RTKs) c-Met, Ron, and c-Src with low-micromolar IC(50)s. The enantiomers of 3 were resolved by HPLC on a chiral phase. Both enantiomers showed a comparable inhibition of the HGF-induced autophosphorylation of c-Met and of subsequent cell migration.
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