The authors optimized a small series of 4-acyl pyrroles, which they further analyzed by ITC, X-ray crystallography, selectivity studies, the NCI60 cell-panel, and GI50 determinations for several cancer cell lines.
[Journal of Medicinal Chemistry]
6807162
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apa
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Hügle, M., Regenass, P., Warstat, R., Hau, M., Schmidtkunz, K., Lucas, X., Wohlwend, D., Einsle, O., Jung, M., Breit, B., & Günther, S. (2020). 4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.0c00478 Cite
