Pflieger, Marc; Soennichsen, Melf; Horstick-Muche, Nadine; Yang, Jing; Schliehe-Diecks, Julian; Schoeler, Andrea; Borkhardt, Arndt; Hamacher, Alexandra; Kassack, Matthias U.; Hansen, Finn K.; Bhatia, Sanil; Kurz, Thomas published their research in ChemMedChem in 2021. The article was titled 《Oxa Analogues of Nexturastat A Demonstrate Improved HDAC6 Selectivity and Superior Antileukaemia Activity》.SDS of cas: 36016-38-3 The article contains the following contents:
The acetylome is important for maintaining the homeostasis of cells. Abnormal changes can result in the pathogenesis of immunol. or neurol. diseases, and degeneration can promote the manifestation of cancer. In particular, pharmacol. intervention in the acetylome with pan-histone deacetylase (HDAC) inhibitors is clin. validated. However, these drugs exhibit an undesirable risk-benefit profile due to severe side effects. Selective HDAC inhibitors might promote patient compliance and represent a valuable opportunity in personalised medicine. Therefore, authors envisioned the development of HDAC6-selective inhibitors. During authors lead structure identification, demonstrated that an alkoxyurea-based connecting unit proves to be beneficial for HDAC6 selectivity and established the synthesis of alkoxyurea-based hydroxamic acids. Herein, authors report highly potent N-alkoxyurea-based hydroxamic acids with improved HDAC6 preference compared to nexturastat A. Authors further validated the biol. activity of these oxa analogs of nexturastat A in a broad subset of leukemia cell lines and demonstrated their superior anti-proliferative properties compared to nexturastat A. The experimental part of the paper was very detailed, including the reaction process of N-tert-Butoxycarbonylhydroxylamine(cas: 36016-38-3SDS of cas: 36016-38-3)
N-tert-Butoxycarbonylhydroxylamine(cas: 36016-38-3) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.SDS of cas: 36016-38-3
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