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Synthesis and Characterization of a Click-Assembled 18-Atom Macrocycle That Displays Selective AXL Kinase Inhibitory Activity
dc.contributor.author | Cruz López, Olga María | |
dc.contributor.author | Franco Montalbán, Francisco | |
dc.date.accessioned | 2020-01-10T10:05:18Z | |
dc.date.available | 2020-01-10T10:05:18Z | |
dc.date.issued | 2019 | |
dc.identifier.citation | Cruz-López, O., Temps, C., Longo, B., Myers, S. H., Franco-Montalban, F., & Unciti-Broceta, A. (2019). Synthesis and Characterization of a Click-Assembled 18-Atom Macrocycle That Displays Selective AXL Kinase Inhibitory Activity. ACS omega. | es_ES |
dc.identifier.uri | http://hdl.handle.net/10481/58625 | |
dc.description.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-d]pyrimidine core. The resulting macrocycle was functionalized further into a multicyclic analog that displays selective inhibitory activity against the receptor tyrosine kinase AXL. | es_ES |
dc.description.sponsorship | O.C.-L. and B.L. thank Spain Ministry of Education, Culture and Sport and the Erasmus + Traineeship programme for funding, respectively. C.T. thanks the CMVM for a Principal’s Scholarship. F.F. acknowledges support from Universidad de Granada. SHM and AU-B are grateful to Scottish Power and CRUK for funding. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | American Chemical Society | es_ES |
dc.rights | Atribución-NoComercial 3.0 España | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc/3.0/es/ | * |
dc.title | Synthesis and Characterization of a Click-Assembled 18-Atom Macrocycle That Displays Selective AXL Kinase Inhibitory Activity | es_ES |
dc.type | journal article | es_ES |
dc.rights.accessRights | open access | es_ES |
dc.identifier.doi | 10.1021/acsomega.9b03525 |