AI Article Synopsis
- Researchers are expanding the structure-activity relationship (SAR) of quinoline compounds within the dihydropyrrolopyrazole series.
- Compound 15d, also known as LY2109761, has shown antitumor efficacy combined with good oral bioavailability.
- The study validates using pharmacokinetic/pharmacodynamic (PK/PD) approaches in vivo as effective for assessing tumor inhibition and potential antitumor efficacy.
Article Abstract
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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| http://dx.doi.org/10.1021/jm701199p | DOI Listing |
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