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    A Second Generation 2-Methoxyestradiol Prodrug Is Effective Against Barrett's Adenocarcinoma in a Mouse Xenograft Model

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    Issue Date
    2016-01-27
    Author
    Kambhampati, Suman
    Rajewski, Roger A.
    Tanol, Mehmet
    Haque, Inamul
    Das, Amlan
    Bangerjee, Snigdha
    Jha, Saheli
    Burns, Douglas
    Reyes, Emma Borrego-Diaz
    Van Veldhuizen, Peter J.
    Banerjee, Sushanta K.
    Publisher
    American Association for Cancer Research
    Type
    Article
    Article Version
    Scholarly/refereed, author accepted manuscript
    Metadata
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    Abstract
    2-Methoxyestradiol (2-ME2) is an endogenous metabolite of estradiol. In preclinical models, 2-ME2 is effective against different types of tumors. Unfortunately, only low systemic concentrations of 2-ME2 can be achieved following oral administration, even after very high doses are administered to patients. In an effort to solve this problem we have now synthesized and tested a new prodrug of 2-ME2 that is water soluble due to a bio-reversible hydrophilic group added at the 3-position and more effectively resists metabolic inactivation due to an ester moiety added to mask the 17-position alcohol. We are reporting here for the first time that this double prodrug of 2-ME2 is effective as an antiproliferative and anti-cancer agent for both in vitro and in vivo studies against Barrett's esophageal adenocarcinoma (BEAC), and provided greater potency than 2-ME2 in inhibiting the growth of BEAC xenografts. Finally, studies indicate that, like 2-ME2, the 2-ME2-PD1 exhibits anticancer effect through possible disruption of microtubule-network.
    Description
    This is the author's accepted manuscript. The original is available at http://mct.aacrjournals.org/content/12/3/255
    URI
    http://hdl.handle.net/1808/20074
    DOI
    https://doi.org/10.1158/1535-7163.MCT-12-0777
    Collections
    • Pharmaceutical Chemistry Scholarly Works [287]
    Citation
    Kambhampati, S., R. A. Rajewski, M. Tanol, I. Haque, A. Das, S. Banerjee, S. Jha, D. Burns, E. Borrego-Diaz, P. J. Van Veldhuizen, and S. K. Banerjee. "A Second-Generation 2-Methoxyestradiol Prodrug Is Effective against Barrett's Adenocarcinoma in a Mouse Xenograft Model." Molecular Cancer Therapeutics 12.3 (2013): 255-63. http://dx.doi.org/10.1158/1535-7163.MCT-12-0777

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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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