- Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1)
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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
- Nie, Zhe,Feher, Victoria,Natala, Srinivasa,McBride, Christopher,Kiryanov, Andre,Jones, Benjamin,Lam, Betty,Liu, Yan,Kaldor, Stephen,Stafford, Jeffrey,Hikami, Kouki,Uchiyama, Noriko,Kawamoto, Tomohiro,Hikichi, Yuichi,Matsumoto, Shin-Ichi,Amano, Nobuyuki,Zhang, Lilly,Hosfield, David,Skene, Robert,Zou, Hua,Cao, Xiaodong,Ichikawa, Takashi
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p. 3662 - 3666
(2013/07/05)
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- Identification of novel, potent and selective inhibitors of Polo-like kinase 1
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A series of pyrimidodiazepines was identified as potent Polo-like kinase 1 (PLK1) inhibitors. The synthesis and SAR are discussed. The lead compound 7 (RO3280) has potent inhibitory activity against PLK1, good selectivity against other kinases, and excell
- Chen, Shaoqing,Bartkovitz, David,Cai, Jianping,Chen, Yi,Chen, Zhi,Chu, Xin-Jie,Le, Kang,Le, Nam T.,Luk, Kin-Chun,Mischke, Steve,Naderi-Oboodi, Goli,Boylan, John F.,Nevins, Tom,Qing, Weiguo,Chen, Yingsi,Wovkulich, Peter M.
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p. 1247 - 1250
(2012/03/26)
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- POLO-LIKE KINASE INHIBITORS
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Compounds of the following formula are provided for use with kinases: (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates use
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Page/Page column 414-415
(2009/05/29)
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- HALO-SUBSTITUTED PYRIMIDODIAZEPINES
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The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
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Page/Page column 70
(2009/12/28)
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