Boron organometallic compounds are mainly known for their great value in organic synthesis to construct biaryls in Suzuki couplings, for arylations of olefins, for C-S, CO , and C-N couplings or as organometallic catalysts. Herein, using arylboronic acids (Ar-B(OH) 2) as a illustrative case, we review the applications of these highly versatile molecules which expands much beyond their commonly perceived uses. Seeing primarily as "mere" intermediates in organic synthesis and organometallic catalysis, this review shows many examples of their uses in other areas of chemistry and seeks therefore to contribute to awaken scientists to the wide range of new possibilities that have been opened to boronorganic compounds, which have acted indeed as very versatile and attractive chemicals with much desirable characteristics such as safety, stability, and [a] N. de
Molecules containing an (cyanovinyl)arene moiety are known as tyrphostins because of their ability to inhibit proteins from the tyrosine kinase family, an interesting target for the development of anticancer and trypanocidal drugs. In the present work, (E)-(cyanovinyl)benzeneboronic acids were synthesized by Knoevenagel condensations without the use of any catalysts in water through a simple protocol that completely avoided the use of organic solvents in the synthesis and workup process. The in vitro anticancer and trypanocidal activities of the synthesized boronic acids were also evaluated, and it was discovered that the introduction of the boronic acid functionality improved the activity of the boronic tyrphostins. In silico target fishing with the use of a chemogenomic approach suggested that tyrosine-phosphorylation-regulated kinase 1a (DYRK1A) was a potential target for some of the designed compounds.
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