Medicinal Chemistry Profiling of Monocyclic 1,2‐Azaborines

• DOI: 10.1002/cmdc.201700047
• Publication Date: 2017-02-09T03:22:56Z
• Authors: Peng Zhao; David O. Nettleton; Rajeshri G. Karki; Frédéric J. Zécri; Shih‐Yuan Liu
• Keywords: Profiling (computer programming)

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 comparison with their corresponding carbonaceous analogues, but the context a CDK2 inhibitor, also biological activity better vivo oral bioavailability. This proof‐of‐concept study establishes viability as novel pharmacophore distinct pharmacological profiles that can help address challenges associated drug development research.