CAS: 1418033-25-6; N-((6-(Hydroxyamino)-6-Oxohexyl)Oxy)-3,5-Dimethylbenzamide

该化合物是一种化学化合物,在医学化学领域,特别是其潜在的治疗用途方面引起注意,被定性为某些蛋白性血管的选择性抑制剂,在细胞生长,分化和新陈代谢等各种细胞过程中发挥着关键作用,该化合物的结构通常具有有助于其生物活动和选择性的特定功能组别.LMK-235已经研究过其对癌症细胞系的影响,表明通过干扰癌症发展所必需的信号路径来抑制肿瘤生长的能力.此外,其溶性与稳定性等药源动力特性对于其作为药物候选者的效力非常重要.研究继续探索其全部潜力,包括其行动机制和可能的副作用,使其成为正在进行的药物开发的一个关注对象.

结构式图片

物理性质

MSDS等安全信息

欧盟法规

C&L通报

上下游产品

CAS号1101114-27-5 6-((1,3-dioxois... | CAS号1418032-61-7 benzyl 6-(1,3-d... | CAS号78277-26-6 6-溴己酸苄酯

合成工艺路线路线简述

  • 合成目标产物 Lmk-235 主要起始原料 Benzyl 6-Bromohexanoate
  • (文献来源)合成步骤主要原料 Benzyl 6-Bromohexanoate
📜6-(Aminooxy)-N-(Benzyloxy)Hexanamide置于4-二甲氨基吡啶,Palladium 10% On Activated Carbon,氢气,1,2-二氯乙烷体系中,用 四氢呋喃,二氯甲烷 用作溶剂,20.0 °C,100.0 Kpa 条件下,反应 28.0H,反应生成N-[[6-(羟基氨基)-6-氧代己基]氧基]-3,5-二甲基-苯甲酰胺
参考文献:Histone Deacetylase (Hdac) Inhibitors With A Novel Connecting Unit Linker Region Reveal A Selectivity Profile For Hdac4 And Hdac5 With Improved Activity Against Chemoresistant Cancer Cells
标题:Histone Deacetylase (Hdac) Inhibitors With A Novel Connecting Unit Linker Region Reveal A Selectivity Profile For Hdac4 And Hdac5 With Improved Activity Against Chemoresistant Cancer Cells
摘要:The Synthesis And Biological Evaluation Of New Potent Hydroxamate-Based Hdac Inhibitors With A Novel Alkoxyamide Connecting Unit Linker Region Are Described. Biological Evaluation Includes Mtt And Cellular Hdac Assays On Sensitive And Chemoresistant Cancer Cell Lines As Well As Hdac Profiling Of Selected Compounds. Compound 191 (Lmk235) (N-((6-(Hydroxyamino)-6-Oxohexyl)Oxy)-3,5-Dimethylbenzamide) Showed Similar Effects Compared To Vorinostat On Inhibition Of Cellular Hdacs In A Pan-Hdac Assay But Enhanced Cytotoxic Effects Against The Human Cancer Cell Lines A2780,Cal27,Kyse510,And Mda-Mb231. Subsequent Hdac Profiling Yielded A Novel Hdac Isoform Selectivity Profile Of 19I In Comparison To Vorinostat Or Trichostatin A (Tsa). 19I Shows Nanomolar Inhibition Of Hdac4 And Hdac5,Whereas Vorinostat And Tsa Inhibit Hdac4 And Hdac5 In The Higher Micromolar Range.
Doi:10.1021/jm301254Q

海关参考信息

其他信息查阅

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

实用工具

⚠️全国化工行业净网倡议书
📋制造商识别码
📖 海关编码查询
📝MSDS生成器

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: Hansen FK, Sumanadasa SD, Stenzel K, Duffy S, Meister S, Marek L, Schmetter R, Kuna K, Hamacher A, Mordmüller B, Kassack MU, Winzeler EA, Avery VM, Andrews KT, Kurz T. Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. Eur J Med Chem. 2014 Jul 23;82:204-13. doi: 10.1016/j.ejmech.2014.05.050. Epub 2014 May 22. doi: 10.1021/jm301254q. Epub 2013 Jan 8.

合成参考文献


参考文献:10.1021/jm301254q
摘要:Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T. Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem. 2013 Jan 24;56(2):427–36. doi: 10.1021/jm301254q.
参考文献:10.1016/j.neuropharm.2021.108893
摘要:Rein B, Conrow-Graham M, Frazier A, Cao Q, Yan Z. Inhibition of histone deacetylase 5 ameliorates abnormalities in 16p11.2 duplication mouse model. Neuropharmacology. 2022 Feb 15;204():108893. doi: 10.1016/j.neuropharm.2021.108893.
📝 需求与反馈
尽可能描述清楚需求与问题信息
×

通知