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

  • Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083.
Zhe Nie  1 ,  Victoria Feher ,  Srinivasa Natala ,  Christopher McBride ,  Andre Kiryanov ,  Benjamin Jones ,  Betty Lam ,  Yan Liu ,  Stephen Kaldor ,  Jeffrey Stafford ,  Kouki Hikami ,  Noriko Uchiyama ,  Tomohiro Kawamoto ,  Yuichi Hikichi ,  Shin-ichi Matsumoto ,  Nobuyuki Amano ,  Lilly Zhang ,  David Hosfield ,  Robert Skene ,  Hua Zou ,  Xiaodong Cao ,  Takashi Ichikawa
Affiliations
  • 1. Takeda California, 10410 Science Center Drive, San Diego, CA 92121, USA.
PMID: 23664874 DOI: 10.1016/j.bmcl.2013.02.083
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.