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Chemistry and biology of curacin A

Wipf, P and Reeves, JT and Day, BW (2004) Chemistry and biology of curacin A. Current Pharmaceutical Design, 10 (12). 1417 - 1437. ISSN 1381-6128

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Many natural and synthetic compounds bind to tubulin, an ubiquitous globular protein that provides the building blocks for the cellular microtubule network that controls chromosome segregation during mitosis, vesicle movements, intracellular transport of organelles, ciliar and flagellar movement, and maintenance of cell shape. Since the isolation of the antimitotic marine natural product curacin A in 1994, synthetic work on this colchicine-site binding agent has been intense, but only recently have synthetic derivatives been identified that match its potency for tubulin polymerization inhibition and its high level of growth inhibition in cancer cell lines. In addition to several total synthesis efforts, combinatorial libraries were constructed using solution phase and fluorous scavenging approaches. Low water-solubility and lack of chemical stability represent strong detriments for the clinical development of curacin A, but synthetic analogs with improved bioavailability might ultimately probe the paradigm for anticancer efficacy of colchicine-site tubulin binding agents. © 2004 Bentham Science Publishers Ltd.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Wipf, Ppwipf@pitt.eduPWIPF
Reeves, JT
Day, BW
Date: 13 May 2004
Date Type: Publication
Journal or Publication Title: Current Pharmaceutical Design
Volume: 10
Number: 12
Page Range: 1417 - 1437
DOI or Unique Handle: 10.2174/1381612043384853
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 1381-6128
Article Type: Review
MeSH Headings: Animals; Antineoplastic Agents--chemistry; Antineoplastic Agents--metabolism; Antineoplastic Agents--pharmacology; Binding Sites--drug effects; Binding Sites--physiology; Cell Line, Tumor; Cyclopropanes--chemistry; Cyclopropanes--metabolism; Cyclopropanes--pharmacology; Humans; Structure-Activity Relationship; Thiazoles--chemistry; Thiazoles--metabolism; Thiazoles--pharmacology; Tubulin--metabolism
PubMed ID: 15134491
Date Deposited: 30 Jan 2014 18:14
Last Modified: 02 Feb 2019 15:57


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