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    Potent immunosuppressive agents, derivatives and uses

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    8841285.pdf (3.019Mb)
    Date
    2014-09-23
    Author
    Romo, Daniel
    Liu, Jun
    Choi, Nam Song
    Shi, Zonggao
    Low, Woon-kai
    Dang, Yongjun
    Schneider-poetsch, Tilman
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    Abstract
    Provided herein include compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drugs mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof. Moreover, the analogs, like pateamine A, are valuable molecular probes for evaluation of eukaryotic translation initiation and as lead compounds for development of improved anticancer agents.
    URI
    https://hdl.handle.net/1969.1/177080
    Subject
    514/183
    540/467
    A61P 35/00
    C07D 277/28
    C07D 513/08
    C07D 277/56
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    • Texas A&M University Patents
    Citation
    Romo, Daniel; Liu, Jun; Choi, Nam Song; Shi, Zonggao; Low, Woon-kai; Dang, Yongjun; Schneider-poetsch, Tilman (2014). Potent immunosuppressive agents, derivatives and uses. United States. Patent and Trademark Office; Texas A&M University. Libraries. Available electronically from https : / /hdl .handle .net /1969 .1 /177080.

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