Schaeker-Huebner, Linda; Warstat, Robin; Ahlert, Heinz; Mishra, Pankaj; Kraft, Fabian B.; Schliehe-Diecks, Julian; Schoeler, Andrea; Borkhardt, Arndt; Breit, Bernhard; Bhatia, Sanil; Huegle, Martin; Guenther, Stefan; Hansen, Finn K. published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads》.SDS of cas: 17696-11-6 The article contains the following contents:
Multitarget drugs are an emerging alternative to combination therapies. In three iterative cycles of design, synthesis, and biol. evaluation, we developed a novel type of potent hybrid inhibitors of bromodomain, and extra-terminal (BET) proteins and histone deacetylases (HDACs) based on the BET inhibitor XD14 and well-established HDAC inhibitors. The most promising new hybrids, 49 and 61, displayed submicromolar inhibitory activity against HDAC1-3 and 6, and BRD4(1), and possess potent antileukemia activity. 49 induced apoptosis more effectively than the combination of ricolinostat and birabresib (1:1). The most balanced dual inhibitor, 61, induced significantly more apoptosis than the related control compounds 62 (no BRD4(1) affinity) and 63 (no HDAC inhibition) as well as the 1:1 combination of both. Addnl., 61 (I) was well tolerated in an in vivo zebrafish toxicity model. Overall, our data suggest an advantage of dual HDAC/BET inhibitors over the combination of two single targeted compounds In the experiment, the researchers used 8-Bromooctanoic acid(cas: 17696-11-6SDS of cas: 17696-11-6)
8-Bromooctanoic acid(cas: 17696-11-6) acid is used in the synthesis of 8-(N-Methyl-4,4′-bipyridinyl)- octanoic acid. 8-Mercaptooctanoic acid was prepared from 8-bromooctanoic acid. And 8-Bromooctanoic Acid is a useful compound for sonodynamic therapy.SDS of cas: 17696-11-6
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary