A HTS screen for CCR1 antagonists afforded a novel sub-micromolar hit 5 containing a pyrazole core. In this report the design, optimization, and SAR of novel CCR1 antagonists based on a pyrazole core motif is presented. Optimization led to the advanced candidate compounds (S)-16q and (S)-16r with 250-fold improved CCR1 potency, excellent off-target selectivity and attractive drug-like properties.
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| http://dx.doi.org/10.1016/j.bmcl.2018.11.015 | DOI Listing |
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Article Synopsis
- * CCR1, CCR3, and CCR5 are receptors that enhance NSCLC cells' migration and invasion, making them potential targets for therapy.
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