CAS: 137218-25-8; 2-(Trifluoromethoxy)Phenylacetonitrile

相似化合物

220239-67-8 1427502-10-0 41429-22-5

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CAS号220239-67-8 2-(三氟甲氧基)苯乙酸

2-三氟甲氧基苯甲酸置于lithium Aluminium Tetrahydride,硫酸,四丁基氟化铵,三溴化磷体系中,用 四氢呋喃,二氯甲烷,乙腈 用作溶剂,化学反应 4.0H,反应生成邻三氟甲氧基苯乙腈
参考文献:Synthesis And Selective Anticancer Activity Evaluation Of 2-Phenylacrylonitrile Derivatives As Tubulin Inhibitors
标题:Synthesis And Selective Anticancer Activity Evaluation Of 2-Phenylacrylonitrile Derivatives As Tubulin Inhibitors
摘要:研究目的 本研究旨在用 2-苯基丙烯腈合成 13 个系列的新型衍生物,评估它们在体内和体外的抗肿瘤活性. 与 2-苯基丙烯腈合成 13 个系列的新型衍生物,评估其体内和体外抗肿瘤活性,并获得新型微管蛋白抑制剂. 获得新型微管蛋白抑制剂. 研究方法 通过 Knoevenagel 缩合法合成了 13 个系列的 2-苯基丙烯腈衍生物,并在体内和体外评估了它们的抗肿瘤活性. 缩合合成了 13 个系列的 2-苯基丙烯腈衍生物,并用 Mtt 法测定了它们的抗增殖活性. 用流式细胞仪分析细胞周期和细胞凋亡.定量细胞迁移 用 24 孔 Boyden 室进行.蛋白质通过 用 Elisa 试剂盒检测微管组装的体外动力学. 试剂盒检测微管组装的体外动力学.分子对接由 Discovery Studio (Ds) 2017 客户端在线工具完成. 结果 在这些衍生物中,化合物 1G2A 对 Hct116 和 Bel-7402 具有很强的抑制活性. 对hct116(ic50 = 5.9 Nm)和bel-7402(ic50 = 7.8 Nm)细胞具有很强的抑制活性.化合物 1G2A 的选择性抗增殖活性和特异性均优于包括紫杉醇在内的所有阳性对照药物. 包括紫杉醇在内的所有阳性对照药物相比,化合物 1G2A 表现出更好的选择性抗增殖活性和特异性.化合物 1G2A 可抑制 Hct116 和 Bel-7402 细胞的增殖,使其停滞在细胞周期的 G2/m 期,抑制 Hct116 和 Bel-7402 细胞的迁移. 抑制 Hct116 和 Bel-7402 细胞的迁移以及细胞集落的形成.化合物 1G2A 对 Hct116 和 Bel-7402 细胞表现出卓越的微管蛋白聚合抑制活性. Bel-7402 细胞表现出优异的小管蛋白聚合抑制活性.分子对接分析结果表明,1G2A 可抑制微管蛋白,从而发挥抗癌作用. 小管蛋白,从而发挥抗癌作用. 结论 化合物 1G2A 在体内和体外都显示出了突出的抗肿瘤活性,有望进一步开发成高效的抗肿瘤药物. 有可能被进一步开发成对正常组织毒性小的高效抗肿瘤药. 对正常组织毒性小的高效抗肿瘤药物.
Doi:10.2174/0109298673263854231009063053

专利信息

专利号:US-4822903-A
优先权日:1981-05-15
标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof
发明人：JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT
权利人:RHONE POULENC SPEC CHIM
摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.

专利号:US-6090805-A
优先权日:1997-06-18
标 题 :Tocolytic oxytocin receptor antagonists
发明人：WILLIAMS PETER D; SPARKS MICHELLE A; BELL IAN; PERLOW DEBRA S; STAUFFER KENNETH; FREIDINGER ROGER M
权利人:MERCK & CO INC
摘要:This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.

专利号:US-5968938-A
优先权日:1997-06-18
标 题 :Piperazine oxytocin receptor antagonists
发明人：WILLIAMS PETER D; SPARKS MICHELLE A; BELL IAN; GUARE JR JAMES P; FREIDINGER ROGER M
权利人:MERCK & CO INC
摘要:This invention relates to certain novel piperazine compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.