Structure-based optimization identified novel furyl-containing 2,4-diarylaminopyrimidine analogues as ALK/ROS1 dual inhibitors with anti-mutation effects.
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DOI: 10.1016/j.ejmech.2021.113259
Abstract: Aiming to develop ALK/ROS1 dual inhibitors overcoming ceritinib-resistant G1202R mutant, a dedicated structure-guided modification campaign was conducted based on ALK co-crystal structures. Twenty eight diarylaminopyrimidine (DAAP) analogues possessing furan or tetrahydrofuran group were designed and… read more here.
Keywords: alk ros1; diarylaminopyrimidine; compound; ros1 dual ... See more keywords