Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma

Baishan Jiang(Harvard University), Jie Jiang(Harvard University), Ines H. Kaltheuner(University of Bonn), Amanda Balboni Iniguez(Broad Institute), K. Anand(University of Bonn), Fleur M. Ferguson(Harvard University), Scott B. Ficarro(Harvard University), Bo Kyung A. Seong(Broad Institute), Ann Katrin Greifenberg(University of Bonn), Sofia Dust(University of Bonn), Nicholas Kwiatkowski(Harvard University), Jarrod A. Marto(Harvard University), Kimberly Stegmaier(Broad Institute), Tinghu Zhang(Harvard University), Matthias Geyer(University of Bonn), Nathanael S. Gray(Harvard University)
European Journal of Medicinal Chemistry
April 20, 2021
10.1016/j.ejmech.2021.113481
Cited by 51Open Access
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