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The cytotoxicity of these compounds were valuated by MTT and SRB methods using three cancer cell lines: HL-60, A-549, P-388. Cyclo-shikonin, and cyclo-alkannin have high cytotoxicity against HL-60.The chiral center of side chain has no effect on their activity. 2- 1-(Acetyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (105) has strong inhibition effect on P-388 cells. 2- 1-(isooctyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (108) and 2- 1-(2-furoyloxy-4-methyl-3-pentenyl -5, 8-dihydroxy-1, 4-naphthoquinone (112) have high inhibition on A-549.Shikonin (1), alkannin (2), and their derivatives have the structural features of a planar chromophores and short side chain. We examined the ability to inhibit the telomerase.

抗肿瘤活性初步筛选测试采用小鼠白血病P-388肿瘤细胞和人肺癌A-549肿瘤细胞进行,结果表明侧链羟基的手性对抗肿瘤活性无明显影响;有数个化合物具有很好的体外抑制活性,特别是化合物2-(1-异辛酰氧基-4-甲基-3-戊烯基)-5,8-二羟基-1,4-萘醌(108)和2-[1-(2-呋喃甲酰氧基)-4-甲基-3-戊烯基]-5,8-二羟基-1,4-萘醌(112)体外显示对人肺癌A-549肿瘤细胞有强效;2-(1-乙酰氧基-4-甲基-3-戊烯基)-5,8-二羟基-1,4-萘醌(105)对小鼠白血病P-388肿瘤细胞有强效;环紫草素和环异紫草素对人白血病HL-60细胞有强烈抑制作用。

We have had the extensive studies on theα-acetyl-α-carbamoyl ketene--acetals and its further applications, for example, their adols condensations with aldehydes giveα-alkenoyl-α-carbamoyl ketene--acetals which can be utilized as the 1,5-bielectronic five-carbon components to react with various binucleophlilic species in a [5+1] annulation.

我们小组在以前的工作中对α-乙酰基-α-胺甲酰基二硫缩烯酮在合成中的应用进行了深入的研究,如与醛缩合生成α-烯酰基-α-胺甲酰基二硫缩烯酮,将其作为1,5-双亲电五碳合成子的[5+1]成环策略等。

The epoxidation of of various olefins was carried out using LDH-F with Mg/Al=5 as the catalyst and H2O2 and benzonitrile as the oxidants. This catalytic system has excellent catalytic activity. The conversion and selectivity are both above 95% when using styrene, indene, allyl alcohol, and allyl chloride as the substrates.

以Mg/Al=5的LDH-F为催化剂,H2O2和苯甲腈为氧化剂对不同官能团化烯烃进行环氧化反应,结果表明,此催化体系具有良好的催化性能,在苯乙烯、茚、丙烯醇和烯丙基氯环氧化反应中转化率和选择性均在95%以上。

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现主要产品:HH—01杀菌剂 HH—02有机分散剂HH—03阳离子淀粉 HH—04木署阳离子淀粉 HH—05 经纱上浆变性淀粉同时还代理销售德国贝克化学公司系列产品主要产品消泡剂:E640 、T50 表面施胶剂:A281、A288 、K532,农药/医药/兽药中间体多种产品(对溴苯酚对溴甲苯溴仿 1-溴庚烷柠檬酸三乙酯 1,2,3-三溴丙烷 3-氯-4-氟溴苯对溴乙苯 4-溴-2-氯苯胺溴乙酸乙酯 2-溴-5-氯甲苯 3-溴丙酸甲酯 1,6-二溴己烷 1-溴-4-硝基苯邻甲氧基苯甲醛溴乙酸丙酯对氟甲苯溴代十二烷对碘甲苯四溴乙烷溴代叔丁烷柠檬酸三丁酯 2-溴氯苯间羟基苯甲醛溴丁烷 2-溴丙酸黎芦醛溴已烷间溴三氟甲苯对溴苯腈对溴乙苯邻溴甲苯溴代环已烷溴代环戊烷糠溴酸马来酸二丁酯溴丙烯乳酸乙酯间溴苯胺间溴苯甲醚邻氟苯酚邻氟苯腈对氨基苯甲醛对溴苯胺对溴苯甲醛对溴苯甲酸)等在相关单位得到了大量推广,与客户建立了良好的合作关系,得到了用户的赞誉。

About 12.9%-27% of applied amount of 14C-metsulfuron-methyl was mineralize d to 14CO2 through opening 14C-triazine ring in soils tested after 180 days of the incubation.

4在整个培养试验期间(180d),14C-甲磺隆在7种土壤中通过三嗪杂环开环矿化为14CO2的量约占引入量的12.9-27.0%,其在碱性土壤中更难被矿化为14CO2。

Methods and Results— We conducted a meta-analysis to compare aprotinin,-aminocaproic acid, and tranexamic acid with placebo and head to head on 8 clinical outcomes from 138 trials.

方法和结果:我们对138个试验中的8项临床数据进行了一项荟萃分析来比较蛋白酶抑制剂、-氨基己酸、氨甲环酸(反式对氨甲基环己烷羧酸)和安慰剂的作用。

Dioxymethylene Mandelic Acid was synthesized by Benzo[1,3]- dioxole which was prepared from catechol .

以邻苯二酚为原料制备胡椒环,然后再从胡椒环合成3,4—亚甲二氧基苯乙醇酸,研究了第二步的反应温度、反应时间以及物料摩尔比对收率的影响,该步反应收率为88%。

Some useful fluorine-containing intermedi-ates were synthesized by the reaction of activated methylenecompounds or silyl enol ether with 2,2-dihydropolyfluoro-alkanoates or 2-hydropolyfluoroalk-2-enoates in the presenceof different bases.

进一步研究表明,在氢化钠的作用下,苯乙腈,苄基苯基甲酮也可以与2-氢多氟-2-烯酸乙酯发生亲核加成反应,苄基苯基甲酮的加成中间体经多聚磷酸环化,得到了间位氟烷基取代的α-萘酚衍生物。

A compound of formula wherein R1 is hydrogen, halo or methoxy; R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is carboxy, tetrazolyl, or -CONHSO2R where R is methyl, ethyl, phenyl, 2,5-dimethylisoxazolyl or trifluoromethyl; T is -CH2- or -SO2-; and ring A is 3-chlorophenyl, 4-chlorophenyl, 3-trifluoromethylphenyl, 3,4-dichlorophenyl, 3,4-difluorophenyl, 3-fluoro-4-chlorophenyl, 3-chloro-4-fluorophenyl or 2,3-dichloropyrid-5-yl; or a pharmaceutically acceptable salt or prodrug thereof, as well as pharmaceutical compositions containing them are described and claimed.

本发明涉及一种式化合物,其中R 1 是氢原子、卤素或甲氧基;R 2 是氢原子、卤素、甲基、乙基或甲氧基;R 3 是羧基、四唑基或-CONHSO 2 R 4 ,其中R 4 是甲基、乙基、苯基、2,5-二甲基异∴唑基或三氟甲基;T是-CH 2 -或-SO 2 -;环A是3-氯苯基、4-氯苯基、3-三氟甲基苯基、3,4-二氯苯基、3,4-二氟苯基、3-氟-4-氯苯基、3-氯-4-氟苯基或2,3-二氯吡啶-5-基;或其药用允许的盐或前药,还包括所阐述和要求权利的含有它们的药用组合物。

Part II: The structural modification of norcantharidin and the discovery and applications of NCS-DMSO combinatorial system: A series of derivatives of 5,6-dehydronorcantharidin was transferred into their corresponding 5,6-epoxynorcantharidin derivatives with Oxone, and finally 14 new compounds have been synthesized; and we also discover the novel combinatorial system NCS-DMSO to make N-aromatic substituted norcantharidin amic acids to their corresponding imides in high yields.

利用十分廉价的Oxone为氧化剂,成功的得到了14个5,6-环氧去甲斑蝥素系列衍生物;同时我们意外地发现了NCS-DMSO组合体系可以使去氢去甲斑蝥素酰胺类化合物实现分子内脱水而生成亚胺类化合物,首次发现和运用该全新的组合体系实现了该类反应。

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