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Separation of Cdc25 dual specificity phosphatase inhibition and DNA cleaving activities in a focused library of analogs of the antitumor antibiotic Dnacin

Wipf, P and Hopkins, CR and Phillips, EO and Lazo, JS (2002) Separation of Cdc25 dual specificity phosphatase inhibition and DNA cleaving activities in a focused library of analogs of the antitumor antibiotic Dnacin. Tetrahedron, 58 (32). 6367 - 6372. ISSN 0040-4020

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Abstract

Biological evaluation of 96 analogs and synthetic intermediates of the naphthyridinomycin-type antitumor antibiotic Dnacin led to the identification of several low-micromolar inhibitors of dual specificity phosphatases, specifically Cdc25A1, Cdc25B2, and VHR, as well as the tyrosine phosphatase PTP1B. While the parent Dnacins are potent DNA cleavage agents, most of the analog structures, even those that retained significant phosphatase inhibitory activities, did not lead to plasmid DNA cleavage. Thus, the DNA-targeting and the phosphatase-inhibitory activities of Dnacins can be assigned to different pharmacophores. © 2002 Elsevier Science Ltd. All rights reserved.


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Details

Item Type: Article
Status: Published
Creators/Authors:
CreatorsEmailPitt UsernameORCID
Wipf, Ppwipf@pitt.eduPWIPF
Hopkins, CR
Phillips, EO
Lazo, JS
Date: 5 August 2002
Date Type: Publication
Journal or Publication Title: Tetrahedron
Volume: 58
Number: 32
Page Range: 6367 - 6372
DOI or Unique Handle: 10.1016/s0040-4020(02)00636-1
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 0040-4020
Date Deposited: 18 Jul 2014 21:00
Last Modified: 26 Oct 2019 14:55
URI: http://d-scholarship.pitt.edu/id/eprint/22263

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