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, Jie Jiang, Ines H. Kaltheuner, Amanda Balboni Iniguez, K. Anand, Fleur M. Ferguson, Scott B. Ficarro, Bo Kyung A. Seong, Ann Katrin Greifenberg, Sofia Dust, Nicholas Kwiatkowski, Jarrod A. Marto, Kimberly Stegmaier, Tinghu Zhang, Matthias Geyer, Nathanael S. Gray