α–ω Alkenyl-bis-S-Guanidine Thiourea Dihydrobromide Affects HeLa Cell Growth Hampering Tubulin Polymerization

Cancer is going to be the first cause of mortality worldwide in the 21th century. It is considered a multifactorial disease that results from the combined influence of many genetic aberrations, leading to abnormal cell proliferation. As microtubules are strongly implicated in cellular growth, they represent an important target for cancer treatment. The well-known microtubule-targeting agents (MTAs) including paclitaxel, colchicine and vinca alkaloids are commonly used in the treatment of various cancers. However, adverse effects and drug resistance are major limitations in their clinical use. To find new candidates able to induce microtubule alteration with reduced toxic effects or drug resistance, we studied a small new series of derivatives that present imidazolinic, guanidinic, thioureidic and hydrazinic groups ( 1 – 9 ). All the compounds were tested for their antitumor activity against a panel of six tumoral cell models. In particular, compound 8 (nonane-1,9-diyl-bis-S-amidinothiourea dihydrobromide) showed the lowest IC₅₀ value against HeLa cells, together with a low cytotoxicity for normal cells. This compound was able to induce the apoptotic mitochondrial pathway and inhibited tubulin polymerization with a similar efficacy to vinblastine and nocodazole. Taken together, these promising biological properties make compound 8 useful for the development of novel therapeutic approaches in cancer treatment.     

两种高效低成本咪唑啉类缓蚀剂的研制

为了缓解油田设备因腐蚀引起的问题,实验通过有机合成方法,用苯甲酸(油酸)和三乙烯四胺及氯化苄合成得到咪唑啉季铵盐缓蚀剂,经过油酸咪唑啉季铵盐缓蚀剂与苯甲酸咪唑啉季铵盐缓蚀剂的复配后,通过静态失重法进行评价。结果表明这类缓蚀剂的最佳加药浓度为30 mg·L-1,此时两种酸类咪唑啉季铵盐含量比为2∶3时的缓蚀效率可以达到97.4%;主剂(苯甲酸∶油酸=2∶3)与硫脲、乌洛托品、乙酰苯胺按比例10∶5∶2∶1复配缓蚀效率可以达到98.4%,符合油田生产需求。     

一种新型抗高温酸化缓蚀剂的制备与性能评价

硫脲、多乙烯多胺、油酸按照质量比0.2∶1∶2,通过缩合脱水反应合成出了一种油酸硫脲基咪唑啉,并复配表面活性剂、吡啶、醛、炔醇等,得到一种新型抗高温酸化缓蚀剂LX-1,对缓蚀剂的缓蚀性能、相容性、抗温性能进行评价。结果表明,缓蚀剂的缓蚀性能良好,LX-1加量为0.6%时,缓蚀率达到95%,腐蚀速率达0.015 mm/a;与地层离子及各种化学剂相容性好;能抗高温90℃,盐酸浓度20%时,腐蚀速率0.023 mm/a,缓蚀率89.0%。     

脱氢枞基咪唑啉的制备及结构表征

对脱氢枞酸二乙烯三胺盐(Ⅱ)进行热重分析,提出了一种制备脱氢枞基咪唑啉(Ⅳ)的方法。将脱氢枞酸(Ⅰ)用带水剂二甲苯溶解,滴加到热的二乙烯三胺(DETA)中进行高温液液短接触脱水缩合反应,得到产品;DETA既是反应物,又是产品的不良溶剂,还起到调控反应温度的作用;二甲苯受热快速蒸发并将反应生成的水带离反应体系。反应结束后,该产品易于从反应混合物中冷却结晶析出、过滤分离,经元素分析、红外光谱、紫外光谱、1HNMR及13CNMR核磁共振谱的波谱结构表征确证。反应物料比可以改变反应体系的温度,进而对产品产率与外观色泽有较大的影响;在化合物Ⅰ的用量为30 mmol、DETA与化合物Ⅰ的物质的量之比为15.7、反应温度为210℃的条件下,产品产率为86.0%。     

Synthesis,Corrosion Inhibition Performance and Biodegradability of Novel Alkyl Hydroxyethyl Imidazoline Salts

New alkyl hydroxyethyl imidazoline salts were synthesized via a high pressure process with imidazoline and dimethyl carbonate, and their chemical structure were confirmed using mass spectral fragmentation and FTIR spectroscopic analysis. In addition, several quaternary ammonium salts with new counterions (formic acid, acetic acid and lactic acid) were also synthesized by ion exchange reaction of methyl carbonate quaternary ammoniums with the corresponding acids. These new compounds reduced the surface tension of water to a minimum value of approximately 27 mN m^?1 at a concentration of 8.72 × 10^?5 mol L^?1. They also show efficient corrosion inhibition performances and could significantly inhibit the corrosion of mild steel in acid solutions. It was also found that the biological degradation of these imidazoline surfactants was greater than 98 % after 7 days.     

新型肉桂基咪唑啉缓蚀剂的合成及其对盐酸介质中Q235钢的缓蚀性能

目前,有关用肉桂酸和有机胺合成咪唑啉衍生物及其合成产物的缓蚀性能与机理研究未见介绍。利用肉桂酸和二乙烯三胺脱水反应生成咪唑啉衍生物,采用失重法、电化学方法、量子化学计算研究了合成缓蚀剂对Q235钢的缓蚀性能和机理。结果表明,新型肉桂基咪唑啉的缓蚀率随缓蚀剂浓度的增大而升高,＂-31mol／LHCl中缓蚀剂浓度为800m...     

油松籽油酸洗缓蚀剂的合成与应用

以油松籽油、二乙烯三胺、氯化苄为原料,合成了咪唑啉季铵盐缓蚀剂Y-1,用失重法、极化曲线法评价了Y-1及其与硫脲复配后的新型缓蚀剂的缓蚀性能.结果表明:缓蚀剂Y-1在盐酸体系中对A20钢有很好的缓蚀效果,由Y-1和硫脲复配的新型缓蚀剂在柠檬酸体系中对A20钢的缓蚀效率在99.65％以上,并且二者都具有很好的热稳定性;缓...     

水溶性咪唑啉类缓蚀剂的合成及性能研究

针对油田注水开发过程中存在的腐蚀问题,合成了水溶性的咪唑啉类缓蚀剂LRX,利用静态挂片法和极化曲线法考察了其缓蚀性能。结果表明,在苯甲酸与二乙烯三胺的摩尔比为1∶1.4,咪唑啉中间体与氯乙酸的摩尔比1∶1.5,季铵化温度控制在60℃,反应时间4 h时,合成的咪唑啉类缓蚀剂LRX为阳极型缓蚀剂,对20#钢的缓蚀率达85%;合成的咪唑啉类缓蚀剂LRX与阻垢剂HEDP复配后,在缓蚀和阻CaCO3垢性能方面具有良好的协同效应。     

高取代度阳离子淀粉改性棉纤维用于活性染料无盐染色的研究

本文以取代度为0.6的高取代度季铵型阳离子淀粉为阳离子化试剂,对棉纤维进行阳离子化改性,用于活性染料无盐染色.通过改性棉纤维表面Zeta电位变化和染料等温吸附曲线对无盐染色促染机理进行研究,对有盐染色和无盐染色中的染料色光、色牢度和染色纤维折皱回复性和强度性能进行比较,从而对高取代度季铵型阳离子淀粉的应用性能进行综合评...     

温度对咪唑啉缓蚀剂成环程度及缓蚀性能的影响

以二乙烯三胺和油酸为原料,在一定反应时间、不同反应温度下合成了系列咪唑啉缓蚀剂。应用红外、紫外分光光度计对合成缓蚀剂进行了分析鉴定,测定了不同反应温度下得到产物的酸值,并用电化学极化曲线法研究了产物的缓蚀性能。结果表明,反应温度越高成环化越高,产物缓蚀性能越好,并且烷基酰胺化和烷基酰胺环化同时进行;极化曲线表明添加该缓蚀剂均可不同程度抑制阴阳极反应,属于混合型缓蚀剂。