Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 7, Pages 2302-2306Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm701199p
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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.
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