Optimization of a dihydropyrrolopyrazole series of transforming growth factor-β type I receptor kinase domain inhibitors: Discovery of an orally bioavailable transforming growth factor-β receptor type I inhibitor as antitumor agent
In our continuing effort to expand the SAR of the quinoline domain of dihydropyrrolopyrazole series, we have discovered compound 15d, which demonstrated the antitumor efficacy with oral bioavailability. This effort also demonstrated that the PK/PD in vivo target inhibition paradigm is an effective approach to assess potential for antitumor efficacy. The dihydropyrrolopyrazole inhibitor 15d (LY2109761) is representative of a novel series of antitumor agents.
Li, Hong-Yu,McMillen, William T.,Heap, Charles R.,McCann, Denis J.,Yan, Lei,Campbell, Robert M.,Mundla, Sreenivasa R.,King, Chi-Hsin R.,Dierks, Elizabeth A.,Anderson, Bryan D.,Britt, Karen S.,Huss, Karen L.,Voss, Matthew D.,Wang, Yan,Clawson, David K.,Yingling, Jonathan M.,Sawyer, J. Scott
p. 2302 - 2306
(2008/12/20)
QUINOLINYL-PYRROLOPYRAZOLES
A compound according to formula II and the pharmaceutically acceptable salts thereof and the method of treating cancer in a patient in need thereof by administration of said compound.
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Page 7
(2010/02/07)
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