Loading...
The Synthesis and Evaluation of Flavone and Isoflavone Chimeras of Novobiocin and Derrubone
Mays, Jared R. Hill, Stephanie A. Moyers, Justin T. Blagg, Brian S. J.
Mays, Jared R.
Hill, Stephanie A.
Moyers, Justin T.
Blagg, Brian S. J.
Citations
Altmetric:
Abstract
The natural products novobiocin and derrubone have both demonstrated Hsp90 inhibition and structure–activity relationships have been established for each scaffold. Given these compounds share several key structural features, we hypothesized that incorporation of elements from each could provide insight to structural features important for Hsp90 inhibition. Thus, chimeric analogues of novobiocin and derrubone were constructed and evaluated. These studies confirmed that the functionality present at the 3-position of the isoflavone plays a critical role in determining Hsp90 inhibition and suggests that the bicyclic ring system present in both novobiocin and derrubone do not share similar modes of binding.
Description
Date
2010-01-01
Journal Title
Journal ISSN
Volume Title
Publisher
Elsevier
Collections
Research Projects
Organizational Units
Journal Issue
Keywords
Hsp90, Novobiocin, Derrubone, Anticancer
Citation
Mays, J. R., Hill, S. A., Moyers, J. T., & Blagg, B. S. J. (2010). The Synthesis and Evaluation of Flavone and Isoflavone Chimeras of Novobiocin and Derrubone. Bioorganic & Medicinal Chemistry, 18(1), 249. http://doi.org/10.1016/j.bmc.2009.10.061