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Lookup NU author(s): Angelica Mariani, Dr Mandeep Atwal, Ka Lee, Professor Caroline AustinORCiD
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The TOP2 poison etoposide has been implicated in the generation of secondary malignancies during cancer treatment. Structural similarities between TOP2 isoforms challenge the rational design of isoform-specific poisons to further delineate these processes. Herein, we describe the synthesis and biological evaluation of a focused library of etoposide analogues, with the identification of two novel small molecules exhibiting TOP2B-dependent toxicity. Our findings pave the way toward studying isoform-specific cellular processes by means of small molecule intervention.
Author(s): Mariani A, Bartoli A, Atwal M, Lee KC, Austin CA, Rodriguez R
Publication type: Article
Publication status: Published
Journal: Journal of Medicinal Chemistry
Year: 2015
Volume: 58
Issue: 11
Pages: 4851-4856
Print publication date: 11/06/2015
Online publication date: 06/05/2015
ISSN (print): 0022-2623
ISSN (electronic): 1520-4804
Publisher: American Chemical Society
URL: http://dx.doi.org/10.1021/acs.jmedchem.5b00473
DOI: 10.1021/acs.jmedchem.5b00473
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