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Bioactivation of Isoxazole-Containing Bromodomain and Extra-Terminal Domain (BET) Inhibitors
- Noah R. Flynn,
- Michael D. Ward,
- Mary A. Schleiff,
- Corentine M. C. Laurin,
- Rohit Farmer,
- Stuart J. Conway,
- Gunnar Boysen,
- S. Joshua Swamidass and
- Grover P. Miller
The 3,5-dimethylisoxazole motif has become a useful and popular acetyl-lysine mimic employed in isoxazole-containing bromodomain and extra-terminal (BET) inhibitors but may introduce the potential for bioactivations into toxic reactive metabolites. A...