AI Article Synopsis
- 5-Aminopyrazole-4-carboxamide served as a new structural basis to replace a component in a known inhibitor targeting calcium-dependent protein kinase-1.
- The resulting compounds showed very effective (low nanomolar) inhibition against the targeted enzymes.
- The best inhibitors were not only selective but also demonstrated low toxicity and effectiveness in cell proliferation tests.
Article Abstract
5-Aminopyrazole-4-carboxamide was used as an alternative scaffold to substitute for the pyrazolopyrimidine of a known "bumped kinase inhibitor" to create selective inhibitors of calcium-dependent protein kinase-1 from both and . Compounds with low nanomolar inhibitory potencies against the target enzymes were obtained. The most selective inhibitors also exhibited submicromolar activities in cell proliferation assays and were shown to be non-toxic to mammalian cells.
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Source |
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3908674 | PMC |
| http://dx.doi.org/10.1021/ml400315s | DOI Listing |
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