Literature DB >> 28181424

Medicinal Chemistry Profiling of Monocyclic 1,2-Azaborines.

Peng Zhao1, David O Nettleton2, Rajeshri G Karki2, Frédéric J Zécri2, Shih-Yuan Liu1.   

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.
© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  BN heterocycle; CDK2 inhibitors; azaborines; drug discovery; solubility

Mesh：

Substances：

Year:  2017        PMID： 28181424      PMCID： PMC5654323          DOI： 10.1002/cmdc.201700047

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  34 in total

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  16 in total

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5.  1,2-Azaborine's Distinct Electronic Structure Unlocks Two New Regioisomeric Building Blocks via Resolution Chemistry.

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9.  Post-Assembly Reactivity of N-Aryl Iminoboronates: Reversible Radical Coupling and Unusual B-N Dynamic Covalent Chemistry.

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10.  Selectivity in the Elaboration of Bicyclic Borazarenes.

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