-transparent.png){kind=logo}
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. 2012
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA. mike.curtin@abbott.com
In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity, a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was conducted and revealed a series of thienopyridine ureas with promising activity against the Aurora kinases. Modification of the diphenyl urea and C7 moiety of these compounds provided potent inhibitors with good pharmacokinetic profiles that were efficacious in mouse tumor models after oral dosing. Compound 2 (ABT-348) of this series is currently undergoing Phase I clinical trials in solid and hematological cancer populations.
Related Publications
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
January 2014,
ChemMedChem,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
January 2010,
Biochimica et biophysica acta,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
December 2004,
Nature reviews. Cancer,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
February 2010,
Critical reviews in oncology/hematology,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
April 2010,
Anti-cancer drugs,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
September 2009,
Bioorganic & medicinal chemistry letters,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
September 2008,
Bioorganic & medicinal chemistry letters,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
September 2004,
Expert opinion on investigational drugs,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
October 2009,
Bioorganic & medicinal chemistry letters,
Michael L Curtin, and
Robin R Frey, and
H Robin Heyman, and
Niru B Soni, and
Patrick A Marcotte, and
Lori J Pease, and
Keith B Glaser, and
Terrance J Magoc, and
Paul Tapang, and
Daniel H Albert, and
Donald J Osterling, and
Amanda M Olson, and
Jennifer J Bouska, and
Zhiwen Guan, and
Lee C Preusser, and
James S Polakowski, and
Kent D Stewart, and
Chris Tse, and
Steven K Davidsen, and
Michael R Michaelides
May 2009,
Journal of medicinal chemistry,
