Abstract
Follow my lead! NSC 670224, previously shown to be toxic to Saccharomyces cerevisiae at low micromolar concentrations, potentially acts via a mechanism of action related to that of tamoxifen (NSC 180973), breast cancer drug. The structure of NSC 670224, previously thought to be a 2,4-dichloro arene, was established as the 3,4-dichloro arene, and a focused library of analogues were synthesized and biologically evaluated.
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Antineoplastic Agents, Hormonal / chemistry*
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Antineoplastic Agents, Hormonal / pharmacology
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Benzyl Compounds / chemical synthesis
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Benzyl Compounds / chemistry*
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Cell Death
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Cyclohexanes / chemical synthesis
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Cyclohexanes / chemistry*
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Dose-Response Relationship, Drug
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Female
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Saccharomyces cerevisiae / drug effects
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Small Molecule Libraries / chemistry*
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Small Molecule Libraries / pharmacology
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Tamoxifen / chemistry
Substances
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(2-(4-tert-butyl-1-(3,4-dichloro-benzyl)-cyclohexyloxy)-ethyl)-dimethyl-amine hydrochloride
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Antineoplastic Agents, Hormonal
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Benzyl Compounds
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Cyclohexanes
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Small Molecule Libraries
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Tamoxifen