Semisynthetic aurones and methods of use thereof
A semi-synthetic, auran technology, applied in the application field of semi-synthetic aurone with anti-tumor activity, auran inhibits the growth of cancer cells in patients in need
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[0090] Prior to this example, certain aurones were known, but were not considered practical antineoplastic agents due to their limited potency and uncertain biological, cellular targets. In particular, published work has led to semi-synthetic aurones with varying levels of antitumor activity: with 2-(coumarin-4-yl)methylene and 2-(furan-2-yl)methylene Benzofuran-3(2 / / )-one is active against human leukemia K562 cells; benzofuran-3(2 / / )-one with 2-(piperazin-l-yl)methylene is active against A solid tumor cell line has IC50 values in the low micromolar range; The cell proliferation of -231 cell line has inhibitory effect. However, the relative potency among these heteroaryl-substituted aurones, and in these cases the specific biological target(s) remains unknown.
[0091] With this in mind, structure-activity (SAR) studies involving modifications of the C-6 hydroxyl and C-2 benzylidene subunits found in many naturally occurring aurones were performed. See Scenario 1 below. ...
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