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Issue 2, 2010
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Cytotoxic sugar analogues of an optimized novobiocin scaffold

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Abstract

Studies on the natural product, novobiocin, have elucidated specific modifications that increase Hsp90 inhibition. Through diversification of the sugar appendage, coumarin core and benzamide side chain of novobiocin, structurally unique scaffolds have been synthesized. These structural adaptations have produced potent cytotoxic agents, such as KU135, which are prepared more simply than those that contain the noviose sugar. These analogues have been evaluated against two cancer cell lines and demonstrated low micromolar anti-proliferative activity.

Graphical abstract: Cytotoxic sugar analogues of an optimized novobiocin scaffold

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Publication details

The article was received on 30 Apr 2010, accepted on 17 Jun 2010 and first published on 30 Jul 2010


Article type: Concise Article
DOI: 10.1039/C0MD00063A
Citation: Med. Chem. Commun., 2010,1, 165-170
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    Cytotoxic sugar analogues of an optimized novobiocin scaffold

    A. C. Donnelly, H. Zhao, B. Reddy Kusuma and B. S. J. Blagg, Med. Chem. Commun., 2010, 1, 165
    DOI: 10.1039/C0MD00063A

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