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Medicinal Chemistry Profiling of Monocyclic 1,2-Azaborines.

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.

SUBMITTER: Zhao P

PROVIDER: S-EPMC5654323 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature

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Medicinal Chemistry Profiling of Monocyclic 1,2-Azaborines.

Zhao Peng P Nettleton David O DO Karki Rajeshri G RG Zécri Frédéric J FJ Liu Shih-Yuan SY

ChemMedChem 20170221 5

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 he ...[more]

PMID: 28181424

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