Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 12, Pages 3662-3666Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.02.083
Keywords
TAK-960; PLK1 inhibitor; Structure-based drug design; Antitumor activity; Multidrug resistance
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Using structure-based drug design, we identified and optimized a novel series of pyrimidodiazepinone PLK1 inhibitors resulting in the selection of the development candidate TAK-960. TAK-960 is currently undergoing Phase I evaluation in adult patients with advanced solid malignancies. (C) 2013 Elsevier Ltd. All rights reserved.
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