106 research outputs found

    Synthesis of A83586C/citropeptin hybrid and synthetic studies toward azinothricin

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    The Azinothricin family of cyclodepsipeptides are a class of antitumour antibiotics whose antitumour properties are attributed to their ability to selectively repress the expression of genes essential for the progression of the cell cycle from G1 to S phase. They have been shown to inhibit E2F transcription factors, which are critical regulators of mammalian cellular proliferation. This biological observation has made them a potentially important new therapeutic target for the control of proliferative diseases, such as cancer. An asymmetric total synthesis of an A83586C-citropeptin hybrid is presented in this thesis, along with a synthetic route to the azinothricin cyclodepsipeptide. The A83586C- citropeptin hybrid will serve as a useful intracellular probe that will provide valuable insights into the mechanism of the antitumour action of this class, which may contribute to a greater understanding of cancer biology. The cyclodepsipeptide components of these molecules have been assembled via a 2+2+2 -fragment condensation strategy and a HATU-mediated macrolactamisation. In the case of the A83586C-citropeptin hybrid, a chemoselective coupling was performed between the fully elaborated N-hydroxybenzotriazole activated ester and the citropeptin cyclodepsipeptide

    The Survey of the Administrators of the Telemedicine Hospital (<i>N</i> = 31).

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    <p>The Survey of the Administrators of the Telemedicine Hospital (<i>N</i> = 31).</p

    The Survey of the Intention of Medical Workers from Primary Medical Institutions (<i>N</i> = 186).

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    <p>The Survey of the Intention of Medical Workers from Primary Medical Institutions (<i>N</i> = 186).</p

    The Survey of the Satisfaction of Patients Who Had Experienced the Telemedicine Service (<i>N</i> = 360).

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    <p>The Survey of the Satisfaction of Patients Who Had Experienced the Telemedicine Service (<i>N</i> = 360).</p

    The Survey of Physicians’ Satisfaction with the Experience of Telemedicine in Gansu Provincial Hospital (<i>N</i> = 95).

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    <p>The Survey of Physicians’ Satisfaction with the Experience of Telemedicine in Gansu Provincial Hospital (<i>N</i> = 95).</p

    The IT infrastructure of telemedicine consultation canter of Gansu.

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    <p>ADSL is Asymmetric Digital Subscriber Line and VPN is Virtual Private Network.</p

    <i>N</i>‑Heterocyclic Carbene-Catalyzed Regio- and Enantioselective C7-Alkylation of 4‑Aminoindoles with α‑Bromoenals

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    The first carbene-catalyzed regio- and enantioselective indole C7-alkylation reaction between 4-aminoindoles and α-bromoenals is disclosed. The corresponding indole products could be obtained in moderate to good yields with good to excellent enantioselectivities. The evaluation of antibacterial activity against Psa revealed that nine of the C7-functionalized indoles exhibited superior inhibitory activities compared to the positive controls TC and BT. Our approach provides an efficient strategy to introduce a chiral chain into the C7 position of indole compounds, with potential applications evaluated in pesticide development

    <b>Proteomic study of nintedanib in gastric cancer cells</b>

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    Nintedanib inhibits proliferation, invasion, and metastasis of gastric cancer cells</p
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