Medicinal Chemistry Profiling of Monocyclic 1,2‐Azaborines
ChemMedChem2017Vol. 12(5), pp. 358–361
Citations Over TimeTop 10% of 2017 papers
Abstract
The first examples of biologically active monocyclic 1,2-azaborines have been synthesized and demonstrated to exhibit not only improved in vitro aqueous solubility in comparison with their corresponding carbonaceous analogues, but in the context of a CDK2 inhibitor, also improved biological activity and better in vivo oral bioavailability. This proof-of-concept study establishes the viability of monocyclic 1,2-azaborines as a novel pharmacophore with distinct pharmacological profiles that can help address challenges associated with solubility in drug development research.
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