CAS: 65300-53-0; 4-(2-(4-Nitrophenoxy)Ethyl)Morpholine

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CAS号3240-94-6 4-(2-氯乙基)吗啉 | CAS号100-02-7 对硝基苯酚 | CAS号110-91-8 吗啉 | CAS号13288-06-7 2-溴乙基 4-硝基苯基醚 | CAS号622-40-2 N-(2-羟乙基)吗啉 | CAS号350-46-9 对氟硝基苯 | CAS号3647-69-6 N-(2-氯乙基)吗啉盐酸盐 | CAS号100-00-5 对硝基氯苯 | CAS号1124-31-8 对硝基(苯)酚钾 | CAS号52481-41-1 4-(2-吗啉基乙氧基)苯胺

2-(4-硝基苯氧基)乙醇置于吡啶,氯化亚砜,Potassium Carbonate,Potassium Iodide体系中,用 1,4-二氧六环,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 6.0H,反应生成 4-(2-(4-硝基苯氧基)乙基)吗啉
参考文献:设计,合成,生物学评估和分子对接研究靶向erα的新型3-芳基-4-苯胺基-2H-铬基-2-酮衍生物作为抗乳腺癌药物.
标题:设计,合成,生物学评估和分子对接研究靶向erα的新型3-芳基-4-苯胺基-2H-铬基-2-酮衍生物作为抗乳腺癌药物.
摘要:雌激素受体(er)在乳腺癌的发展和进程中起着重要作用,并且是抗癌药物发现的主要目标.为了开发新颖的选择性erα调节剂(serm),我们基于先前报道的先导化合物设计并合成了18种新颖的3-芳基-4-苯胺基-2H-色烯-2-酮衍生物.生物学结果表明,与阳性对照他莫昔芬相比,大多数化合物具有有效的erα结合亲和力,并且对mcf-7和ishikawa细胞系具有更好的抗增殖活性.哌啶基取代的化合物(例如16D和18D)分别具有很强的erα结合亲和力和出色的抗增殖活性.化合物18D显示最有效的erα结合亲和力,Rba值为2.83%,16D对mcf-7细胞表现出最佳的抗增殖活性,Ic50值为4.52+/-2.47μm.还进行了进一步的分子对接研究,以研究新合成的化合物与erα的结合模式.所有这些结果以及结构-活性关系(sar)表明,这些具有碱性侧链的3-芳基-4-苯胺基-2H-铬-2-基衍生物可以作为进一步优化新型serm的有前途的线索.
DOI:10.1016/j.Bmcl.2017.04.029

专利信息

专利号:US-4999378-A
优先权日:1987-10-20
标题:Phenylcarboxylic acid derivatives
发明人：FUJII SETSURO; KAWAMURA HIROYUKI; WATANABE SHINICHI
权利人:OTSUKA PHARMA CO LTD
摘要:Phenylcarboxylic acid derivatives having the formula: ##STR1## wherein R 1 and R 2 are each H, halogen, alkyl, haloalkyl, alkanoyl, cycloalkyl, nitro, amino, --O--D--R 5 (D is alkylene, R 5 is H, amino, morpholino, carboxyl, phthalimido, phenyl, epoxy), substituted or unsubstituted phenoxy, substituted or unsubstituted phenylalkylamino, carboxylalkenyl, or both form alkylenedioxy; R 3 is H, --E--R 6 (E is alkylene, R 6 is H, carboxyl, cyano, OH, phenylalkoxy, or halogen-substituted phenyl, or phenylcarbamoyl), --CO--G--R 7 (G is alkylene, R 7 is H, substituted or unsubstituted phenylcarbamoyl), substituted or unsubstituted benzoyl, alkenyl, carbamoyl, phenyl, or halophenyl; R 4 is H or alkyl; A is alkylene, alkylene condensed with cycloalkyl ring, or alkenylene; B is alkylene or alkenylene; l is 0 or 1. Said compounds have fatty acid synthesis-inhibitory activity, cholesterol synthesis-inhibitory activity and are useful as antilipidemic agent, prophylactic and treating agent of artherosclerosis, prophylactic and treating agent of obesity, antidiabetics.