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New inhibitors of the thioredoxin-thioredoxin reductase system based on a naphthoquinone spiroketal natural product lead

Wipf, P and Hopkins, TD and Jung, JK and Rodriguez, S and Birmingham, A and Southwick, EC and Lazo, JS and Powis, G (2001) New inhibitors of the thioredoxin-thioredoxin reductase system based on a naphthoquinone spiroketal natural product lead. Bioorganic and Medicinal Chemistry Letters, 11 (19). 2637 - 2641. ISSN 0960-894X

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Natural products of the naphthoquinone spiroketal structural type served as lead structures for the development of novel inhibitors of the thioredoxin-thioredoxin reductase redox system. The most potent compound in this series inhibited thioredoxin with an IC50 of 350 nM, and many derivatives showed low micromolar activities for growth inhibition against two breast cancer cell lines. © 2001 Elsevier Science Ltd. All rights reserved.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Wipf, Ppwipf@pitt.eduPWIPF
Hopkins, TD
Jung, JK
Rodriguez, S
Birmingham, A
Southwick, EC
Lazo, JS
Powis, G
Date: 8 October 2001
Date Type: Publication
Journal or Publication Title: Bioorganic and Medicinal Chemistry Letters
Volume: 11
Number: 19
Page Range: 2637 - 2641
DOI or Unique Handle: 10.1016/s0960-894x(01)00525-x
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 0960-894X
MeSH Headings: Antineoplastic Agents--chemical synthesis; Antineoplastic Agents--chemistry; Antineoplastic Agents--pharmacology; Cell Division--drug effects; Dioxanes--chemical synthesis; Dioxanes--chemistry; Dioxanes--pharmacology; Drug Screening Assays, Antitumor; Epoxy Compounds--chemical synthesis; Epoxy Compounds--chemistry; Epoxy Compounds--pharmacology; Humans; Naphthalenes; Naphthoquinones--chemical synthesis; Naphthoquinones--chemistry; Naphthoquinones--pharmacology; Spiro Compounds--chemical synthesis; Spiro Compounds--chemistry; Spiro Compounds--pharmacology; Thioredoxin-Disulfide Reductase--antagonists & inhibitors; Thioredoxins--antagonists & inhibitors; Tumor Cells, Cultured
PubMed ID: 11551767
Date Deposited: 13 Feb 2014 18:57
Last Modified: 22 Jun 2021 12:55


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