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Medicinal Chemistry Profiling of Monocyclic 1,2‐Azaborines
Author(s) -
Zhao Peng,
Nettleton David O.,
Karki Rajeshri G.,
Zécri Frédéric J.,
Liu ShihYuan
Publication year - 2017
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201700047
Subject(s) - profiling (computer programming) , chemistry , medicinal chemistry , computer science , operating system
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.