CAS: 7530-27-0; 4-Bromo-2-Chloro-6-Methylphenol

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4-Bromo-2-methylphenol 2-chloro-6-methylphenol 2-chloro-6-methyl-[1,4]benzoquinone 2-chloro-6-methylphenol 5-bromo-1-chloro-2-methoxy-3-methylbenzene 2,6-dimethoxy-3-methylcarbazole

📜2-氯-6-甲酚置于n-溴代丁二酰亚胺(Nbs)体系中,用 溶剂黄146 作为反应溶剂,化学反应生成 4-溴-2-氯-6-甲基苯酚
参考文献:雌激素依赖性疾病的治疗:设计,合成和分析具有亚纳摩尔级ic50的选择性17β-Hsd1抑制剂,以进行原理验证研究.
标题:雌激素依赖性疾病的治疗:设计,合成和分析具有亚纳摩尔级ic50的选择性17β-Hsd1抑制剂,以进行原理验证研究.
摘要:当前用于雌激素依赖性疾病子宫内膜异位症的内分泌治疗剂通常会引起相当大的副作用,因为它们通过全身性地降低雌激素作用而起作用.最近的方法利用了以下事实:血浆中富含的雌激素雌激素(e1)在靶细胞中被17β-羟类固醇脱氢酶1型(17β-Hsd1)激活为高雌激素雌二醇(e2). .17β-Hsd1在子宫内膜异位症中过表达,因此是治疗该疾病的有希望的靶标,并有望减少与靶标相关的副作用.我们最近描述的具有磺酰胺部分的双环取代的羟基苯基亚甲酮类的强抑制剂在17β-Hsd1的生理对手--17βhsd2上具有高分子量和低选择性.我们描述了导致(5-(3,5-二氯-4-甲氧基苯基)噻吩-2-基)(2,6-二氟-3-羟苯基)甲酮20的发现的结构优化,它显示了亚纳摩尔级对17β-Hsd1的ic50以及对2型酶,雌激素受体α和β以及一系列肝cyp酶的高选择性.该化合物在ames Ii分析中既未显示出细胞毒性,也未显示
DOI:10.1016/j.Ejmech.2016.11.004

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.