Discovery of Quinoline‐Derived Trifluoromethyl Alcohols,Determination of Their in vivo Toxicity and Anticancer Activity in a Zebrafish Embryo Model

In this study the rational design, synthesis, and anticancer activity of quinoline‐derived trifluoromethyl alcohols were evaluated. Members of this novel class of trifluoromethyl alcohols were identified as potent growth inhibitors in a zebrafish embryo model. Synthesis of these compounds was carried out with an sp³‐C?H functionalization strategy of methyl quinolines with trifluoromethyl ketones. A zebrafish embryo model was also used to explore the toxicity of ethyl 4,4,4‐trifluoro‐3‐hydroxy‐3‐(quinolin‐2‐ylmethyl)butanoate ( 1 ), 2‐benzyl‐1,1,1‐trifluoro‐3‐(quinolin‐2‐yl)propan‐2‐ol ( 2 ), and trifluoro‐3‐(isoquinolin‐1‐yl)‐2‐(thiophen‐2‐yl)propan‐2‐ol ( 3 ). Compounds 2 and 3 were found to be more toxic than compound 1 ; apoptotic staining assays indicated that compound 3 causes increased cell death. In vitro cell proliferation assays showed that compound 2 , with an LC₅₀ value of 14.14 μm , has more potent anticancer activity than cisplatin. This novel class of inhibitors provides a new direction in the discovery of effective anticancer agents.     

Potent Synergy between Spirocyclic Pyrrolidinoindolinones and Fluconazole against Candida albicans

A spiroindolinone, (1S,3R,3aR,6aS)‐1‐benzyl‐6′‐chloro‐5‐(4‐fluorophenyl)‐7′‐methylspiro[1,2,3a,6a‐tetrahydropyrrolo[3,4‐c]pyrrole‐3,3′‐1H‐indole]‐2′,4,6‐trione, was previously reported to enhance the antifungal effect of fluconazole against Candida albicans. A diastereomer of this compound was synthesized, along with various analogues. Many of the compounds were shown to enhance the antifungal effect of fluconazole against C. albicans, some with exquisite potency. One spirocyclic piperazine derivative, which we have named synazo‐1, was found to enhance the effect of fluconazole with an EC₅₀ value of 300 pM against a susceptible strain of C. albicans and going as low as 2 nM against some resistant strains. Synazo‐1 exhibits true synergy with fluconazole, with an FIC index below 0.5 in the strains tested. Synazo‐1 exhibited low toxicity in mammalian cells relative to the concentrations required for antifungal synergy.     

芳香醛、苯乙酮和对硝基苯胺一锅法合成Mannich碱

在浓盐酸做催化剂的条件下,芳香醛、苯乙酮和对硝基苯胺能够发生Mannich反应,经过提纯得到相应的Mannich碱。用红外光谱对产物的结构进行表征,并研究浓盐酸的使用量、反应温度、反应时间等条件对产率的影响。实验发现在3滴浓盐酸催化下,控温在15~20℃,反应20 h,产率可达60%左右。     

具有优良热氧稳定性的可加工双邻苯二甲腈树脂

通过"一锅法"合成了含芳醚键的低聚双邻苯二甲腈单体,并以4,4'-双(4-氨基苯氧基)二苯砜(p-BAPS)为固化剂获得了具有较高稳定性和热氧稳定性的聚合物树脂。低聚邻苯二甲腈单体制备过程为过量间苯二酚与4'4-二氟二苯甲酮反应,以N,N-二甲基甲酰胺(DMF)/甲苯为溶剂,加入适量K2CO3,最后用4-硝基邻苯二甲腈进行封端。合成的低聚双邻苯二甲腈单体用IR及1H-NMR进行结构表征。该低聚物单体与4,4'-双(4-氨基苯氧基)二苯砜(p-BAPS)进行热交联形成一个密实的热固性材料。通过热重分析和差示扫描量热分析研究该聚合物树脂的固化性能及热氧稳定性,结果表明该聚合物固化温度在450℃左右,在氮气氛下开始分解的温度为330℃,因此该固化物具有优良的热稳定性和氧化稳定性。     

二维色谱测定石脑油中微量含氧化合物

文章采用二维气相色谱测定石脑油及乙烯裂解装置原料中微量含氧化物的含量。二维中心切割(heart-cutting)技术样品中的氧化物组份在非极性柱上预分离后,被切割到极性柱上继续分离,氢火焰离子化检测器检测含氧化合物含量。该方法操作简单,分析时间在20 min以内,重复测定结果的相对标准偏差小于1.8%,方法准确可靠。     

以类水滑石为前驱体制备Ru基CH_4-CO_2重整催化剂

以类水滑石为前驱体,采用共沉淀法制备了不同Ru含量的xRu/Mg(Al)O催化剂(x=1,2,4),采用XRD、H2-TPR和CO脉冲吸附等表征催化剂结构和Ru金属分散度,并评价Ru含量对CH4-CO2重整反应活性与稳定性的影响。XRD与CO脉冲吸附结果表明,Ru含量增加时,还原后Ru金属颗粒的表面活性位数目增加,但分散度降低,Ru金属的粒径增大。活性测试结果表明,Ru质量分数为2%时,催化剂活性最高。Ru质量分数为1%时,催化剂具有较好的稳定性,归属于高分散Ru金属颗粒与Mg(Al)O载体之间的强相互作用。     

固体废物中多环芳烃萃取的前处理技术及测定方法综述

多环芳烃(PAHs)是环境中广泛存在的一类污染物,其存在于水体、大气及土壤介质中,具有种类多及对环境危害大的特点。近年来,PAHs逐渐成为人们研究的重点,虽然国内外已有PAHs的监测技术的分析标准,但是其提取与测定是一个系统的过程,且不断发展和优化。比较了近年来固体废物(如土壤、污泥等)中PAHs的分析过程中所涉及的萃取、净化及测定方法,总结了各种分析方法的优缺点,介绍了一些新的分析技术。     

Corrosion Inhibition and Adsorption Behavior of Sodium Lauryl Ether Sulfate on L80 Carbon Steel in Acetic Acid Solution and Its Synergism with Ethanol

The application of sodium lauryl ether sulfate (SLES) as an anionic surfactant and its synergistic combination with ethanol for inhibition of corrosion of L80 carbon steel in acetic acid solutions were investigated by means of potentiodynamic polarization measurements, scanning electron microscopy (SEM), X‐ray diffraction (XRD), and energy‐dispersive X‐ray (EDX) investigations. The inhibition efficiency increases with an increase in concentration of SLES. The adsorption of SLES on the surface of L80 carbon steel obeys the Freundlich isotherm. SLES acts predominately as an anodic inhibitor. XRD, EDX, and SEM examinations of the electrode surface confirmed the adsorption of SLES on the electrode surface. The addition of ethanol with SLES significantly enhances the inhibition effectiveness and generates a strong synergistic effect.     

New,Non‐quinone Fluorogeldanamycin Derivatives Strongly Inhibit Hsp90

Streptomyces hygroscopicus is a natural producer of geldanamycin. Mutasynthetic supplementation of an AHBA‐blocked mutant with all possible monofluoro 3‐aminobenzoic acids provided new fluorogeldanamycins. These showed strong antiproliferative activity and inhibitory effects on human heat shock protein Hsp90. Binding to Hsp90 in the low nanomolar range was determined from molecular modelling, AFM analysis and by calorimetric studies.