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Updated: Mar 7, 2026

Synthesis of 1,2-Azaborines and the Preparation of Their Protein Complexes with T4 Lysozyme Mutants
Published on: March 25, 2017
Medicinal Chemistry Profiling of Monocyclic 1,2-Azaborines
Peng Zhao1, David O Nettleton2, Rajeshri G Karki2
1Department of Chemistry, Boston College, Chestnut Hill, MA, 02467, USA.
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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