Bellenie, Benjamin R.; Cheung, Kwai-Ming J.; Varela, Ana; Pierrat, Olivier A.; Collie, Gavin W.; Box, Gary M.; Bright, Michael D.; Gowan, Sharon; Hayes, Angela; Rodrigues, Matthew J.; Shetty, Kartika N.; Carter, Michael; Davis, Owen A.; Henley, Alan T.; Innocenti, Paolo; Johnson, Louise D.; Liu, Manjuan; de Klerk, Selby; Le Bihan, Yann-Vai; Lloyd, Matthew G.; McAndrew, P. Craig; Shehu, Erald; Talbot, Rachel; Woodward, Hannah L.; Burke, Rosemary; Kirkin, Vladimir; van Montfort, Rob L. M.; Raynaud, Florence I.; Rossanese, Olivia W.; Hoelder, Swen published the artcile< Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders>, Safety of (R)-Butane-1,3-diol, the main research area is preparation benzimidazolone inhibitor BCL6 interaction repressor lymphoma.
Deregulation of the transcriptional repressor BCL6 enables tumorigenesis of germinal center B-cells, and hence BCL6 has been proposed as a therapeutic target for the treatment of diffuse large B-cell lymphoma (DLBCL). Herein we report the discovery of a series of benzimidazolone inhibitors of the protein-protein interaction between BCL6 and its co-repressors. A subset of these inhibitors were found to cause rapid degradation of BCL6, and optimization of pharmacokinetic properties led to the discovery of 5-((5-chloro-2-((3R,5S)-4,4-difluoro-3,5-dimethylpiperidin-1-yl)pyrimidin-4-yl)amino)-3-(3-hydroxy-3-methylbutyl)-1-methyl-1,3-dihydro-2H-benzo[d]imidazol-2-one (CCT369260), which reduces BCL6 levels in a lymphoma xenograft mouse model following oral dosing.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 6290-03-5 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H10O2, Safety of (R)-Butane-1,3-diol.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts