| Literature DB >> 22695126 |
Michael L Curtin1, H Robin Heyman, Robin R Frey, Patrick A Marcotte, Keith B Glaser, James R Jankowski, Terrance J Magoc, Daniel H Albert, Amanda M Olson, David R Reuter, Jennifer J Bouska, Debra A Montgomery, Joann P Palma, Cherrie K Donawho, Kent D Stewart, Chris Tse, Michael R Michaelides.
Abstract
In an effort to identify kinase inhibitors with dual KDR/Aurora B activity and improved aqueous solubility compared to the Abbott dual inhibitor ABT-348, a series of novel pyrazole pyrimidines structurally related to kinase inhibitor AS703569 were prepared. SAR work provided analogs with significant cellular activity, measureable aqueous solubility and moderate antitumor activity in a mouse tumor model after weekly ip dosing. Unfortunately these compounds were pan-kinase inhibitors that suffered from narrow therapeutic indices which prohibited their use as antitumor agents.Entities:
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Year: 2012 PMID： 22695126 DOI： 10.1016/j.bmcl.2012.05.067
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823