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Raltitrexed(0.5μg\u002F mL)显示典型的凋亡形态,包括核收缩,片段化,染色质浓缩和SGC7901细胞中的凋亡小体。 Raltitrexed阻断细胞周期在G0\u002FG1期,线粒体膜电位降低。 Raltitrexed还可以增加ROS水平,通过激活线粒体诱导caspase-3依赖性细胞凋亡,并增加TS蛋白和mRNA表达水平[3]。 Raltitrexed(1.5 nM)可减少GM00637细胞的数量,选择性诱导基因转换,但不影响DSB诱导的HR或NHEJ [4]。",{"key":249,"value":250},"体内研究","Raltitrexed(0,5,10,11.5,13.5,15mg\u002Fkg b\u002Fw,ip)以剂量依赖性方式增加再吸收胚胎的速率和NTD的鼠模型的生长迟缓。 Raltitrexed(11.5 mg\u002Fkg b\u002Fw)最大限度地抑制胚胎组织中的胸苷酸合成酶(TS)活性,降低dTMP水平,同时增加dUMP水平[2]。",{"key":252,"value":253},"细胞实验","为了评估Raltitrexed对细胞活力和\u002F或生长的影响，将GM00637细胞以每瓶3.3×10 5个细胞的密度接种到25cm 2烧瓶中。二十四小时后，用补充有各种剂量的Raltitrexed的培养基替换培养基，其浓度范围从小于1nM到大于1μM。每个测试剂量使用三个细胞培养瓶。将细胞暴露于Raltitrexed 24小时，此时用不含Raltitrexed的培养基重新培养细胞。用无药物培养基喂养48小时后，收获细胞并计数。将暴露于各种Raltitrexed剂量的细胞的细胞计数与未暴露于Raltitrexed的对照细胞的细胞计数进行比较，作为Raltitrexed对细胞活力和\u002F或生长速率的影响的量度。",{"key":255,"value":256},"动物实验","在实验中使用成年（7-8周，19-20g）C57BL \u002F 6小鼠。将小鼠维持在22℃，12小时光照\u002F天周期，并随意喂食标准小鼠食物和自来水。将雌性小鼠与雄性小鼠交配过夜，并在第二天早晨检查阴道栓。怀孕小鼠中阴道栓的存在被认为是妊娠第0.5天。将怀孕的小鼠随机分成6组，每组10只小鼠。将Raltitrexed溶解于0.9％NaCl中，并在妊娠第7.5天腹膜内注射不同剂量的Raltitrexed（5,10,11.5,13.5,15mg \u002F kg b \u002F w）。对照组在妊娠7.5天以相同体积腹膜内注射0.9％NaCl。在妊娠第11.5天，处死怀孕的小鼠，并在解剖显微镜下检查胚胎。",{"key":258,"value":259},"参考文献","[1].\nZhao H, et al. Raltitrexed Inhibits HepG2 Cell Proliferation via G0\u002FG1 Cell Cycle Arrest. Oncol Res. 2016;23(5):237-48\n[2].\nDong Y, et al. Raltitrexed's effect on the development of neural tube defects in mice is associated with DNA damage, apoptosis, and proliferation. Mol Cell Biochem. 2015 Jan;398(1-2):223-31.\n[3].\nXue S, et al. Raltitrexed induces mitochondrial-mediated apoptosis in SGC7901 human gastric cancer cells. Mol Med Rep. 2014 Oct;10(4):1927-34.\n[4].\nWaldman BC, et al. Induction of intrachromosomal homologous recombination in human cells by raltitrexed, an inhibitor of thymidylate synthase. 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(欧洲)","Xi: Irritant;",{"key":304,"value":305},"风险声明 (欧洲)","R36\u002F38",{"key":307,"value":308},"安全声明 (欧洲)","S26-S36\u002F37\u002F39-S45-S25",{"key":310,"value":311},"危险品运输编码","UN 3265 8\u002FPG 2",{"key":313,"value":314},"WGK德国","3",{"key":316,"value":317},"包装等级","II",{"key":319,"value":320},"危险类别","8","\u003Cp>1. 2,6-二甲基-4(3H)-喹唑啉酮(I)用叔戊酰氧基甲基氯进行N烷化卮再用N-溴代丁二酰亚胺溴化,得到6-(溴甲基)-2-甲基-3-[(叔戊酰氧基)甲基]-4(3H)-喹唑啉酮(Ⅲ).(m)和N-[5-甲氨基噻吩-2-羰基]-L-谷氨酸二乙酯(IV)缩合,生成物V和氢氧化钠的乙醇水溶液在室温下搅拌水解,并同时脱保护基, 然后酸化得到产物.\u003C\u002Fp>\u003Cp>2.3,4-二氢-2,6-二甲基-3-新戊酰氧基甲基\u002F喹唑啉-4-酮的制备\u003C\u002Fp>\u003Cp>在反应瓶中加入3,4-二氢-2,6-二甲基喹唑啉-4-酮(按文献[9]方法制备或外购)3.0g和二甲基甲酰胺50ml,搅拌溶解,在室温搅拌下向该溶液加入氢化钠(NaH)1.08g,将混合物于室温搅拌1h.再加入氯甲基新戊酸酯3.36g溶\u003C\u002Fp>\u003Cp>于二甲基甲酰胺10ml的溶液,混合物于室温搅拌反应18h.然后将反应液倾入饱和食盐水200ml中,用乙醚(50ml×4)提取,合并乙醚层,无水NaSO4干燥.过滤,滤液蒸发至干,剩余物经硅胶柱色谱纯化[洗脱剂:二氯甲烷\u002F乙酸乙酯(体积比9:1)].经后处理,产物再用石油醚(bp60~80 ºC)结晶,得3,4-二氢-2,6-二甲基-3-新戊酰氧基甲基\u002F喹唑啉-4-酮0.92g,mp98~100 ºC.\u003C\u002Fp>\u003Cp>3. 6-溴甲基-3,4-二氢-2-甲基-3-新戊酰氧基甲基喹唑啉-4-酮的制备\u003C\u002Fp>\u003Cp>在反应瓶中加入上述化合物3,4-二氢-2,6-二甲基-3-新戊酰氧基甲基\u002F喹唑啉-4-酮0.92g、四氯\u003C\u002Fp>\u003Cp>化碳50ml、N-溴代琥珀酰亚胺0.624g和过氧苯甲酰0.025g(催化量)搅拌混合,缓慢升温至回流,在回流下搅拌反应2h.冷却至室温将反应液通过装填硅酸镁25h的柱色谱,用四氯化碳洗脱,洗脱液减压下蒸发至干,得固体剩余物6-溴甲基-3,4-二氢-2-甲基-3-新戊酰氧基甲基喹唑啉-4-酮6-溴甲基-3,4-二氢-2-甲基-3-新戊酰氧基甲基喹唑啉-4-酮1.6g,mp144~145 ºC.\u003C\u002Fp>\u003Cp>4.N-[5-(甲基氨基)-2-噻吩甲酰基]-L-谷氨酸二乙酯的制备\u003C\u002Fp>\u003Cp>在反应瓶中加入2-噻吩羧酸300g(2.34mol)、叔丁醇2500ml,搅拌溶解.在保持温度恒定在20~25C下滴加三乙胺325ml(2.34mol),滴毕,再加入二苯基磷酰叠氮化物(DPPA)517ml(2.4mol). 将混合物搅拌回流12h.冷却,黄色反应液倾倒入冰水7000ml中, 产生白色沉淀,过滤#滤饼用水洗净,于35 ºC下真空干燥得2-[N-(叔丁氧羰基)氨基],噻吩431g,收率92%,mp147~148 ºC.\u003C\u002Fp>\u003Cp>在滴液漏斗中加入2-[N-(叔丁氧羰基)氨基]噻吩100g(0.502mol)溶于DMF300ml溶液,将其滴入悬浮于DMF300ml中的NaH23.1g(分散于油中,55%含量,0.53mol) 的悬浮液中(滴加过程中温度不超过5 ºC,并用氩气保护,用冰浴冷却).滴毕,在0~5 ºC继续搅拌30min,再在搅拌下和15 ºC以下滴加甲基碘3.14g(0.50mol).滴毕,再在20 ºC连续搅拌16h.加入水200ml终止反应,用乙醚(1500ml×4)提取,合并乙醚层,用水洗和盐水\u003C\u002Fp>\u003Cp>洗,干燥,过滤,滤液浓缩蒸除溶剂,得2-[N-(叔丁氧羰基)-N-甲基氨基]噻吩的黄色油状物123g,将其用硅胶柱色谱纯化[洗脱剂为己烷\u002F二氯甲烷(体积比1:1)]得精制的2-[N-(叔丁氧羰基)-N-甲基氨基]噻吩油状物83.3g, 收率78%.\u003C\u002Fp>\u003Cp>反应瓶中加入二异丙胺30ml0.21mol)和THF200ml搅拌溶解,在氩气保护下,于-78 ºC滴加1.6mol\u002FL正丁基锂的己烷溶液119ml,滴加过程中应保持温度低于-50 ºC.滴毕,于-78 ºC下搅拌反应30min.然后在低于-60 ºC下滴加2-[N-(叔丁氧羰基)-N-甲基氨基]噻吩40.8g(0.19mol)溶于THF200ml的溶液,滴毕,在-78 ºC继续搅拌反应30min.然后在防潮情况下小心地少量分批加入粉碎的固体CO2200g(4.54mol)( 保持温度低于-50 ºC).将反应混合物慢慢升温至20 ºC.在该温度下搅拌反应过夜.将反应液倒入水2L中,加入粉状柠檬酸调至pH5,过滤出白色沉淀固体,水洗,真空干燥得5-[N-(叔丁氧基羰基)-N-甲基氨基]-2-噻吩羧酸(A)39.8g,收率81%,mp210~211 ºC (分解)\u003C\u002Fp>\u003Cp>在反应瓶中加入上步产物39g(0.152mol)和DMF60ml溶于CH2Cl2 300ml,溶液,搅拌,于30min.内向该混合物加入草酰氯22.9g(0.27mol), 加毕,继续搅拌30min后,将反应液低于30ºC下蒸发至干,得粗制的酰基氯黏性固体在真空下(0.1mmHg)干燥1h.\u003C\u002Fp>\u003Cp>在反应瓶中加入谷氨酸二乙酯盐酸盐36.15g(0.152mol)和CH2Cl2 260ml ,搅拌溶解,在氩气保护下加入三乙胺34.0g(0.24mol), 在冰浴冷却下,冷至10ºC,再加入上述制备的粗制酰基氯溶于CH2Cl2 200ml溶液. 加料时保持温度低于15 ºC ,加毕,于同温度下搅拌反应过夜.得到暗绿色混合物,用水(200ml×2)洗涤,水层(水洗液)用CH2Cl2 400ml提取,合并有机层,干燥,滤去干燥剂的滤液蒸除溶剂得黑色剩余物,将其通过硅胶柱色谱纯化[洗脱剂为0~5%(体积分数)梯度的乙酸乙酯的CH2Cl2溶液],得粗制谷氨酸衍生物74g.在反应瓶中加入谷氨酸衍生物74g和CF3COOH3 50ml,控温20~25 ºC下搅拌反应16h后将CF3COOH3蒸除#剩余物加入NaHCO3水溶液1L, 用CH2Cl2(500ml×3) 提取,合并CH2Cl2层,用无水Na2SO4干燥,过滤,滤液浓缩得油状物,将其油状物经硅胶柱色谱纯化[洗脱剂为10%(体积分数)乙酸乙酯的CH2Cl2溶液],得N-[5-(甲基氨基)-2-噻吩甲酰基]-L-谷氨酸二乙酯33.35g(为黏稠棕色油状物),收率58%.\u003C\u002Fp>\u003Cp>5.N-[[5-[[(1,4-二氢-2-甲基-3-新戊酰氧甲基-4-氧-6-喹唑啉基)甲基]甲氨基]-2-噻吩基]L-谷氨酸二乙酯的制备\u003C\u002Fp>\u003Cp>在反应瓶中加入N-[5-(甲基氨基)-2-噻吩甲酰基]-L-谷氨酸二乙酯1.5g(4.4mmol) 、6-溴甲基-3,4-二氢-2-甲基-3-新戊酰氧基甲基喹唑啉-4-酮1.71g(4.7mmol) 、2,6-二甲基吡啶0.47g(510μl,4.4mol)和DMF26ml,搅拌溶解.该混合物于60 ºC和氩气保护下搅拌反应18h.冷却#混合物在低于40ºC下蒸发至干,余物经硅胶柱色谱纯化(脱剂:1%甲醇的乙酸乙酯溶液),得N-[[5-[[(1,4-二氢-2-甲基-3-新戊酰氧甲基-4-氧-6-喹唑啉基)甲基]甲氨基]-2-噻吩基]L-谷氨酸二乙酯340mg, 收率15%\u003C\u002Fp>\u003Cp>6. N-[[5-[[(1,4-二氢-2-甲基-4-氧-6-喹唑啉基)甲基]甲氨基]-2-噻吩基]羰基]-L-谷氨酸(兰替特噻)的合成\u003C\u002Fp>\u003Cp>在反应瓶中加入N-[[5-[[(1,4-二氢-2-甲基-3-新戊酰氧甲基-4-氧-6-喹唑啉基)甲基]甲氨基]-2-噻吩基]L-谷氨酸二乙酯340mg(0.66mmol)、加入5ml和1mol\u002FLNaOH水溶液6.6ml(6.6mmol),在氩气保护下搅拌反应2h.将反应液过滤,液用2mol\u002FL盐酸调至Ph3.0,生沉淀,沉淀过滤,滤饼用水洗至无卤离子存在.潮湿产物经干燥,得129mg, 收率41%,mp180~184 ºC.\u003C\u002Fp>\u003Cp>\u003C\u002Fp>","2026-08-21T07:51:12.859463Z",false,[325,331,337,343,349,355,361,367,373,378,384,390],{"slug":326,"cid":327,"name":328,"nameZh":329,"cas":330},"785884778195849216","J-1103278-3","Carbasalate calcium","卡巴匹林钙","5749-67-7",{"slug":332,"cid":333,"name":334,"nameZh":335,"cas":336},"785891455125164032","J-29802-2","Pigment Red 48:2","颜料红48:2","7023-61-2",{"slug":338,"cid":339,"name":340,"nameZh":341,"cas":342},"785895952778006528","J-1512648-4","Pigment Red 52:1","颜料红52:1","17852-99-2",{"slug":344,"cid":345,"name":346,"nameZh":347,"cas":348},"785891221192052736","J-1095551-8","Sudan Black B","苏丹黑B","4197-25-5",{"slug":350,"cid":351,"name":352,"nameZh":353,"cas":354},"785894575997718528","J-38085-8","Pigment Red 63:1","颜料红63:1","6417-83-0",{"slug":356,"cid":357,"name":358,"nameZh":359,"cas":360},"785882292210896896","J-1095737-6","Eriochrome Black T","铬黑T","1787-61-7",{"slug":362,"cid":363,"name":364,"nameZh":365,"cas":366},"785881510895947776","J-19811-8","Zincon","锌试剂","62625-22-3",{"slug":368,"cid":369,"name":370,"nameZh":371,"cas":372},"785888734531817472","J-1958301-8","Isoquercitrin","异槲皮苷","21637-25-2",{"slug":374,"cid":375,"name":376,"nameZh":376,"cas":377},"785947418393841664","J-1874835-1","((Perfluorohexyl)ethyl)-2-chloropropenoate","96383-55-0",{"slug":379,"cid":380,"name":381,"nameZh":382,"cas":383},"785893809820012544","J-1427-7","Eptaplatin","依铂","146665-77-2",{"slug":385,"cid":386,"name":387,"nameZh":388,"cas":389},"785872897603276800","J-1993285-5","Pigment Red 81","颜料红81","12224-98-5",{"slug":391,"cid":392,"name":393,"nameZh":394,"cas":395},"785894610575560704","J-1095917-8","Aluminon","铝试剂","569-58-4",1794258903552,"zh-CN",[]]