苯乙烯喹啉衍生物的合成及抗癌活性

以取代的苯胺和反式丁烯醛为原料,在盐酸中反应得到4个2-甲基喹啉衍生物,所得产物再与芳香醛在冰醋酸中回流反应合成了10个苯乙烯喹啉衍生物,收率为64%~78%。所得化合物的结构经1HNMR、MS、IR表征确认,并采用MTT法进行初步体外抗肿瘤活性筛选。结果表明,化合物Ⅱc对A 549和HCT 116细胞均有较高的抑制活性,IC50值分别为9.77和9.66μmol/L,化合物Ⅱd对HCT 116细胞有较高的抑制活性,IC50值为9.80μmol/L。     

Synthesis and antitumor activity of N

摘要：以STX-0119为先导化合物基于生物电子等排原理设计并合成25个N"-苯亚甲基-2-(3-吡啶基)喹啉-4-酰肼衍生物（产率：20.4-42.6%），通过1H NMR、MS、13C NMR确证了产物结构，采用MTT和台盼蓝法以以人乳腺癌MCF-7细胞、人肺癌A549细胞、人慢性粒细胞白血病K562细胞、人急性B淋巴细胞白血病RS4:11细胞为测试细胞株评价了目标化合物的体外抗肿瘤活性。目标化合物Ⅶr表现出最强的抗A549细胞增殖活性（IC50 = 7.42 ± 0.83 μmol/L），目标化合物Ⅶq表现出最强的抗RS4:11细胞增殖活性（IC50 = 2.4 ± 0.17 μmol/L）目标化合物Ⅶl不仅表现出最强的抗MCF-7细胞增殖活性（IC50 = 4.91 ± 0.33 μmol/L），而且也表现出最强抗K562细胞增殖活性（IC50 = 1.24 ± 0.19 μmol/L），分子对接结果显示其发挥抗肿瘤的作用可能与STAT3通路有关，值得进一步深入研究。 关键词：喹啉；酰肼；合成；抗肿瘤；生物电子等排     

2-溴-4’-羟基查尔酮-苯磺酸酯衍生物的合成及抗肿瘤活性

基于药效团拼合原理设计并合成23个未见文献报道的 (E)-4-[3-(2-溴苯基)丙烯酰基]苯基-取代苯磺酸酯衍生物（产率：60.9-80.3%）,通过1HNMR、MS、13CNMR确证了产物结构,采用MTT法以5-氟尿嘧啶和伊马替尼为阳性对照药,以人宫颈癌Hela细胞、人肺癌A549细胞和人慢性粒细胞白血病K562细胞为测试细胞株评价了目标化合物的体外抗肿瘤活性。目标化合物Ⅴp表现出最强的A549细胞增殖抑制活性(半抑制浓度IC50 = 7.53 μmol/L),优于阳性对照药5-氟尿嘧啶(IC50 = 8.1 μmol/L),目标化合物Ⅴt表现出最强的K562细胞增殖抑制活性(IC50 = 4.47 μmol/L),目标化合物Ⅴd表现出最强的Hela细胞增殖抑制活性（IC50 = 4.53 μmol/L）,比阳性对照药5-氟尿嘧啶(IC50 = 13.5 μmol/L)强约3倍。目标化合物Ⅴd对A549细胞（IC50 = 8.0 μmol/L）和K562细胞（IC50 = 7.81 μmol/L）也表现出强的增殖抑制活性,值得进一步深入研究。     

新型熊果酸喹啉衍生物抗肿瘤活性研究

原料为五环三萜类天然产物熊果酸,合成新型熊果酸喹啉衍生物。使用元素分析法、ESIMS、13C NMR等,分析1,3,4-噁二唑衍生物4a-4f,以及熊果酸喹啉酰肼衍生物3a-3f。采用MTT法,对4a-4f、3a-3f进行测试,分析对三种肿瘤细胞株的增殖抑制活性。结果显示,对三种肿瘤细胞株,包括SMMC-77213、HeL、MDA-MB-231,3a-3c都有明显的抑制活性。比对照依托泊苷更强,对SMMC-77213、HeL、MDA-MB-231的IC50值,分别是17.49～19.43μmol/L、0.84～1.19μμmol/L、1.17～1.85μμmol/L。根据抗肿瘤活性结果显示,喹啉基引入熊果酸分子中,羧基修饰为1,3,4-噁二唑基、酰肼基,抗肿瘤活性能够明显增强,酰肼的衍生物为侧链,相比噁二唑的衍生物活性更佳。因此,能够进一步优化熊果酸结构,提升抗肿瘤活性。     

芳香基苦参碱衍生物的合成及抗肿瘤活性

分别以茴香醛、黎芦醛、3,4,5-三甲氧基苯甲醛、2,3,4-三甲氧基苯甲醛为原料,在氢化钠的作用下,与苦参碱发生Claisen-Schimidt缩合反应合成了4个芳香基苦参碱衍生物;采用MTT法测试目标化合物对人结肠癌细胞株HT-29,人胰腺癌细胞株PANC-1的增殖抑制活性。结果表明,合成的芳香基苦参碱衍生物的IC50值分别为27.8、18.0、9.05、13.2μmol/L,苦参碱的IC50值为28.6μmol/L,4个苦参碱衍生物的抗肿瘤活性较苦参碱有所提高。     

吲哚-2-碳酰肼衍生物的合成及抗肿瘤活性评价

以5-氯-吲哚-2-羧酸为原料,设计合成7个全新的吲哚-2-碳酰肼衍生物,并通过~1HNMR、~(13)CNMR和MS进行结构表征。采用四甲基偶氮唑盐(MTT)染色法对化合物的抗人结肠癌细胞(HCT116)、人乳腺癌细胞(MCF-7)和人肺癌细胞(A549)增殖活性进行评价。结果表明,5-氯-N′-((5-氟-1H-吲哚)-3-亚甲基)-1H-吲哚-2-碳酰肼对HCT116细胞具有显著抑制活性,IC_(50)值为7.72μmol/L,同时发现该化合物能够呈浓度依赖方式诱导HCT116细胞凋亡。     

新型苦参碱C-14腙类衍生物的合成及抗肿瘤活性研究

以苦参碱为先导化合物,设计并合成了16个苦参碱腙类衍生物,均采用¹HNMR、¹³CNMR和HR-MS进行了结构表征。通过MTT比色法进行体外抗增殖活性实验,测试了所有目标化合物对人宫颈癌细胞HeLa、人结肠癌细胞HCT116和非小细胞肺癌细胞A549的活性,部分目标化合物表现出比苦参碱更为优越的抗增殖活性,尤其是化合物14-(((4-叔丁基苄基)-1H-吲哚-3-亚甲基)肼亚甲基)苦参碱,其对HeLa、HCT116和A549细胞的IC₅₀值分别为(11.65±0.28)、(9.14±0.81)和(14.48±0.63)μmol/L,在3种细胞中显示出卓越的抗增殖活性,尤其对HCT116细胞的抗增殖活性最强。进一步的细胞周期实验结果显示,目标化合物能够阻滞HCT116细胞在G0/G1期。分子对接结果表明,该化合物与蛋白6QJX存在氢键和π-π堆积作用等相互作用力。     

含噻吩并[3,2-d]嘧啶的查尔酮类化合物的合成和抗增殖活性

运用药物分子片段原理及拼合原理,设计并合成了10个含噻吩并[3,2-d]嘧啶的查尔酮类衍生物,并对该类化合物的体外抗对肿瘤细胞增殖活性进行初步研究。目标化合物的结构通过1H NMR、13C NMR和HRMS (ESI)表征。以人肺腺癌细胞株A549、人肝癌细胞株HepG2和人前列腺癌细胞株PC-3三种肿瘤细胞为测试细胞株,采用MTT法评价了目标化合物的抗增殖活性。体外活性实验表明,10个化合物对三种肿瘤细胞株均具有很好的抑制活性。其中化合物Ⅶh活性突出,对三种肿瘤细胞株的IC50 值分别为0.87 μmol/L、2.43 μmol/L和2.02 μmol/L,优于阳性对照药索拉非尼。含噻吩并[3,2-d]嘧啶的查尔酮类化合物具有很好的抗肿瘤活性,值得进一步研究。     

异海松酸杂环酰胺衍生物的制备及抗癌活性

为了获得结构新型的抗肿瘤药物分子结构,以天然产物异海松酸为母核结构,合成了9个异海松酸基杂环酰胺化合物（Ⅱa～Ⅱi）,其结构经FTIR、1H NMR、13C NMR和TOF-MS分析确证。抗肿瘤活性测试结果表明,所有目标化合物的抗肿瘤活性均比母体化合物异海松酸的活性高,尤其是含有吡嗪杂环的化合物Ⅱd对A375细胞表现出显著的增殖抑制活性,其IC50值为13.34 μmol/L,有望通过进一步结构修饰来提高活性成为异海松酸类抗癌先导化合物。     

芦荟大黄素唑类衍生物的合成及抗肿瘤作用研究

以天然产物芦荟大黄素为先导化合物,设计、合成了6个未见报道的芦荟大黄素唑类衍生物,结构经核磁共振氢谱、碳谱和质谱确证。以5-氟尿嘧啶(5-Fu)为阳性对照药,采用MTT比色法进行化合物抑制人体结肠癌细胞HCT116的体外活性测试。结果表明,大部分目标化合物对结肠癌细胞的抑制活性强于先导化合物芦荟大黄素,其中3-(((1H-1,2,4-三唑-3-基)巯基)甲基)-1,8-二羟基蒽-9,10-二酮、3-(((5-氨基-4H-1,2,4-三唑-3-基)巯基)甲基)-1,8-二羟基蒽-9,10-二酮对HCT116细胞的半数抑制浓度(IC_(50))分别为15. 18、14. 15μmol/L,明显强于阳性对照药5-Fu(IC_(50)为24. 80μmol/L)。     

Insect antifeedant properties of anthranoids from the genusVismia

Vismiones and ferruginins, representatives of a new class of lypophilic anthranoids from the genusVismia were found to inhibit feeding in larvae of species ofSpodoptera, Heliothis, and inLocusta migratoria.     

Direct observation of freeze-thaw instability of latex coatings via high pressure freezing and cryogenic SEM

Despite its industrial importance, the subject of freeze-thaw (F/T) stability of latex coatings has not been studied extensively. There is also a lack of fundamental understanding about the process and the mechanisms through which a coating becomes destabilized. High pressure (2100 bar) freezing fixes the state of water-suspended particles of polymer binder and inorganic pigments without the growth of ice crystals during freezing that produce artifacts in direct imaging scanning electron microscopy (SEM) of fracture surfaces of frozen coatings. We show that by incorporating copolymerizable functional monomers, it is possible to achieve F/T stability in polymer latexes and in low-VOC paints, as judged by the microstructures revealed by the cryogenic SEM technique. Particle coalescence as well as pigment segregation in F/T unstable systems are visualized. In order to achieve F/T stability in paints, latex particles must not flocculate and should provide protection to inorganic pigment and extender particles. Because of the unique capabilities of the cryogenic SEM, we are able to separate the effects of freezing and thawing, and study the influence of the rate of freezing and thawing on F/T stability. Destabilization can be caused by either freezing or thawing. A slow freezing process is more detrimental to F/T stability than a fast freezing process; the latter actually preserves suspension stability during freezing. Presented at the 82nd Annual Meeting of the Federation of Societies for Coatings Technology, October 27–29, 2004 in Chicago, IL. Tied for first place in The John A. Gordon Best Paper Competition.     

Ethanol and (−)-α-Pinene: Attractant Kairomones for Bark and Ambrosia Beetles in the Southeastern US

In 2002–2004, we examined the flight responses of 49 species of native and exotic bark and ambrosia beetles (Coleoptera: Scolytidae and Platypodidae) to traps baited with ethanol and/or (−)-α-pinene in the southeastern US. Eight field trials were conducted in mature pine stands in Alabama, Florida, Georgia, North Carolina, and South Carolina. Funnel traps baited with ethanol lures (release rate, about 0.6 g/day at 25–28°C) were attractive to ten species of ambrosia beetles (Ambrosiodmus tachygraphus, Anisandrus sayi, Dryoxylon onoharaensum, Monarthrum mali, Xyleborinus saxesenii, Xyleborus affinis, Xyleborus ferrugineus, Xylosandrus compactus, Xylosandrus crassiusculus, and Xylosandrus germanus) and two species of bark beetles (Cryptocarenus heveae and Hypothenemus sp.). Traps baited with (−)-α-pinene lures (release rate, 2–6 g/day at 25–28°C) were attractive to five bark beetle species (Dendroctonus terebrans, Hylastes porculus, Hylastes salebrosus, Hylastes tenuis, and Ips grandicollis) and one platypodid ambrosia beetle species (Myoplatypus flavicornis). Ethanol enhanced responses of some species (Xyleborus pubescens, H. porculus, H. salebrosus, H. tenuis, and Pityophthorus cariniceps) to traps baited with (−)-α-pinene in some locations. (−)-α-Pinene interrupted the response of some ambrosia beetle species to traps baited with ethanol, but only the response of D. onoharaensum was interrupted consistently at most locations. Of 23 species of ambrosia beetles captured in our field trials, nine were exotic and accounted for 70–97% of total catches of ambrosia beetles. Our results provide support for the continued use of separate traps baited with ethanol alone and ethanol with (−)-α-pinene to detect and monitor common bark and ambrosia beetles from the southeastern region of the US.     

Methyl 2,4,6-decatrienoates Attract Stink Bugs and Tachinid Parasitoids

Halyomorpha halys (Stål) (Pentatomidae), called the brown marmorated stink bug (BMSB), is a newly invasive species in the eastern USA that is rapidly spreading from the original point of establishment in Allentown, PA. In its native range, the BMSB is reportedly attracted to methyl (E,E,Z)-2,4,6-decatrienoate, the male-produced pheromone of another pentatomid common in eastern Asia, Plautia stali Scott. In North America, Thyanta spp. are the only pentatomids known to produce methyl 2,4,6-decatrienoate [the (E,Z,Z)-isomer] as part of their pheromones. Methyl 2,4,6-decatrienoates were field-tested in Maryland to monitor the spread of the BMSB and to explore the possibility that Thyanta spp. are an alternate host for parasitic tachinid flies that use stink bug pheromones as host-finding kairomones. Here we report the first captures of adult and nymph BMSBs in traps baited with methyl (E,E,Z)-2,4,6-decatrienoate in central Maryland and present data verifying that the tachinid, Euclytia flava (Townsend), exploits methyl (E,Z,Z)-2,4,6-decatrienoate as a kairomone. We also report the unexpected finding that various isomers of methyl 2,4,6-decatrienoate attract Acrosternum hilare (Say), although this bug apparently does not produce methyl decatrienoates. Other stink bugs and tachinids native to North America were also attracted to methyl 2,4,6-decatrienoates. These data indicate there are Heteroptera in North America in addition to Thyanta spp. that probably use methyl 2,4,6-decatrienoates as pheromones. The evidence that some pentatomids exploit the pheromones of other true bugs as kairomones to find food or to congregate as a passive defense against tachinid parasitism is discussed.     

2007～2008年世界塑料工业进展

收集了2007年7月～2008年6月世界塑料工业的相关资料,介绍了2007～2008年国外塑料工业的发展情况,提供了世界塑料产量、消费量及全球各类树脂的需求量及产能情况.按通用热塑性树脂(聚乙烯、聚丙烯、聚苯乙烯、聚氯乙烯、ABS树脂)、工程塑料(尼龙、聚碳酸酯、聚甲醛、热塑性聚酯、聚苯醚)、特种工程塑料(聚苯·硫醚、液晶聚合物、聚醚醚酮)、通用热固性树脂(酚醛、聚氨酯、不饱和聚酯树脂、环氧树脂)不同品种的顺序,对树脂的产量、消费量、供需状况及合成工艺、产品应用开发、树脂品种的延伸及应用的进一步扩展等技术作了详细介绍.     

2005～2006年国外塑料工业进展

收集了2005年7月～2006年6月国外塑料工业的相关资料,介绍了2005—2006年国外塑料工业的发展情况。提供了世界塑料产量、消费量及全球各类树脂生产量以及各国塑料制品的进出口情况。作为对比,介绍了中国塑料的生产情况。按通用热塑性树脂（聚乙烯、聚丙烯、聚苯乙烯、聚氯乙烯、ABS树脂）、工程塑料（聚酰胺、聚碳酸酯、聚甲醛、热塑性聚酯、聚苯醚）、通用热固性树脂（酚醛、聚氨酯、不饱和树脂、环氧树脂）、特种工程塑料（聚苯硫醚、液晶聚合物、聚醚醚酮）的品种顺序,对树脂的产量、消费量、供需状况及合成工艺、产品开发、树脂品种的延伸及应用的扩展作了详细的介绍。