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4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesulfonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors.

Journal of medicinal chemistry - 26 Nov 2009

Dexheimer Thomas S, Gediya Lalji K, Stephen Andrew G, Weidlich Iwona, Antony Smitha, Marchand Christophe, Interthal Heidrun, Nicklaus Marc, Fisher Robert J, Njar Vincent C, Pommier Yves

Abstract excerpt

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is an enzyme that catalyzes the hydrolysis of 3'-phosphotyrosyl bonds. Such linkages form in vivo when topoisomerase I (Top1) processes DNA. For this reason, Tdp1 has been implicated in the repair of irreversible Top1-DNA covalent complexes. Tdp1 inhibitors have been regarded as potential therapeutics in combination with Top1 inhibitors, such as the camptothecin derivatives,...

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Identifiers

PMID: 19883083
DOI: 10.1021/jm901061s
PMCID: PMC2784989

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4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesulfonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors.PMID 19883083Read ↗

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