Synthesis and Characterization of a Click-Assembled 18-Atom Macrocycle That Displays Selective AXL Kinase Inhibitory Activity.

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ID: 80133
2019
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Abstract
A novel macrocyclic construct consisting of a pyrazolopyrimidine scaffold concatenated to a benzene ring through two triazoles has been developed to investigate uncharted chemical space with bioactive potential. The 18-atom macrocycle was assembled via a double copper-catalyzed alkyne-azide cycloaddition (CuAAC) reaction between 1,3-bis(azidomethyl)benzene and a bis-propargylated pyrazolo[3,4-]pyrimidine core. The resulting macrocycle was functionalized further into a multicyclic analog that displays selective inhibitory activity against the receptor tyrosine kinase AXL.
Reference Key
cruzlpez2019synthesisacs Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Cruz-López, Olga;Temps, Carolin;Longo, Beatrice;Myers, Samuel H;Franco-Montalban, Francisco;Unciti-Broceta, Asier;
Journal ACS omega
Year 2019
DOI
10.1021/acsomega.9b03525
URL
Keywords
Cancer Diabetes schizophrenia pde10 inhibitors

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