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Glycosylated analogues of novobiocin, discovered using a broad library of enzymes, have 100-fold improved activity against breast, brain, pancreatic, lung and ovarian cancers and ablated associated off-target activity leading to an up to 2.7 × 10(4) fold increase in selectivity.

Original publication

DOI

10.1039/c1cc13552j

Type

Journal article

Journal

Chem Commun (Camb)

Publication Date

14/10/2011

Volume

47

Pages

10569 - 10571

Keywords

Cell Line, Tumor, DNA Topoisomerases, Type II, Drug Screening Assays, Antitumor, Enzyme Inhibitors, Enzymes, Glycosylation, HSP90 Heat-Shock Proteins, Humans, Novobiocin