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Novobiocin analogues with second-generation noviose surrogates
Zhao, Huiping Blagg, Brian S. J.
Zhao, Huiping
Blagg, Brian S. J.
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Abstract
Hsp90 is a promising therapeutic target for the treatment of cancer. Novobiocin is the first Hsp90 C-terminal inhibitor ever identified and recent structure-activity relationship studies on the noviose sugar identified several commercially available amines as suitable surrogates. In an effort to further understand this region of the molecule, analogues containing various N′-amino substituents were prepared and evaluated against two breast cancer cell lines for determination of their efficacy. Compound 37j manifested the most potent anti-proliferative activity from these studies and induced Hsp90-dependent client protein degradation at mid nano-molar concentrations.
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Date
2013-01-15
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Elsevier
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Keywords
Heat shock protein 90, Hsp90 inhibitors, Novobiocin analogues, Breast cancer
Citation
Zhao, H., & Blagg, B. S. J. (2013). Novobiocin analogues with second-generation noviose surrogates. Bioorganic & Medicinal Chemistry Letters, 23(2), 552–557. http://doi.org/10.1016/j.bmcl.2012.11.022