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Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).

Authors :
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
Source :
Bioorganic & Medicinal Chemistry Letters. Jun2013, Vol. 23 Issue 12, p3662-3666. 5p.
Publication Year :
2013

Abstract

Abstract: 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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
23
Issue :
12
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
89103714
Full Text :
https://doi.org/10.1016/j.bmcl.2013.02.083