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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。

Suitable water-immiscible organic solvents include aromatic hydrocarbons, eg toluene, xylene, naphthalene, tetrahydronaphthalene and methyl naphthalene; chlorinated aromatic hydrocarbons, eg chlorobenzene, fluorobenzene, chloronaphthalene and bromonaphthalene; esters, eg butyl acetate, ethyl acetate, methyl benzoate, ethyl benzoate, benzyl benzoate, butyl benzoate, phenylethyl acetate, butyl lactate, benzyl lactate, diethyleneglycol dipropionate, dimethyl phthalate, diethyl phthalate, dibutyl phthalate, di(2-ethylhexyl) phthalate; alcohols having six or more carbon atoms, eg hexanol, octanol, benzyl alcohol, phenyl ethanol, phenoxy ethanol, phenoxy propanol and phenoxy butanol; ethers having at least 5 carbon atoms, preferably C 5-14 ethers, eg anisole and phenetol; nitrocellulose, cellulose ether, cellulose acetate; low odour petroleum distillates; turpentine; white spirits; naphtha; isopropylbiphenyl; terpene; vegetable oil; mineral oil; essential oil; and natural oil; and mixtures of any two or more thereof.

适用于水互溶的有机溶剂包括芳香族碳氢化合物,如甲苯,二甲苯,萘,四氢萘和甲基萘;氯代芳香族碳氢化合物,如氯苯,氟,氯萘和萘;酯类,如醋酸丁酯,醋酸乙酯,苯甲酸甲酯,苯甲酸乙酯,苄酯,苯甲酸正丁酯,苯,醋酸丁酯乳酸,乳酸苄,二甘醇二丙酸酯,邻苯二甲酸二甲酯,邻苯二甲酸二乙酯,邻苯二甲酸二丁酯,二(2乙基己基)酯;醇有6个或更多碳原子,如己醇,辛醇,苯甲醇,苯乙醇,苯氧基乙醇,丙醇和苯氧基苯氧丁醇;醚至少有5个碳原子,最好荤5-14醚,如苯甲醚和phenetol;硝化棉,纤维素醚,醋酸纤维素,低气味石油蒸馏;松节油;白酒,石脑油isopropylbiphenyl;萜类,植物油,矿物油,挥发油;和天然油,以及任何两个或两个以上其混合物。

A series of novel dendrons with 1,3,5-triazine structure were synthesized by convergent strategy using cyanuric chloride, p-hydroxyazobenzene,β-naphthol, 1-hydroxyanthraquinone, 3,5-dihydroxybenzyl. They were the first generation p-phenyl-azo-phenyloxy-terminated dendron G1.0, the first generation naphthyloxy-terminated dendron G1.0, the first generation naphthyloxy-terminated and 1-anthraquinonoxy-cored dendron G, and the second generation naphthyloxy-terminated dendron G2.0.

以对羟基偶氮苯、β-萘酚为端基,三聚氯氰、3,5-二羟基苄醇为支化单体,1-羟基蒽醌为核心,用收敛法合成了一系列新型结构的含均三嗪环的树枝块:第一代端基为偶氮苯的树枝块G1.0、端基为萘氧基的树枝块G1.0、端基为萘氧基、中心为蒽醌的树枝块G、第二代端基为萘氧基的树枝块G2.0。

A series of long chain alkyl methylnaphthalene sulfonates, including hexyl methylnaphthalene sulfonate, octyl methylnaphthalene sulfonate, decyl methylnaphthalene sulfonate, dodecyl methylnaphthalene sulfonate, and tetradecyl methylnaphthalene sulfonate, was characterized by high performance liquid chromatography and electrospray ionization mass spectrometry. Through a great deal of testing, the analytical conditions were optimized.

采用反相离子对高效液相色谱和电喷雾离子化质谱对系列长链烷基甲基萘磺酸盐,包括己基甲基萘磺酸盐、辛基甲基萘磺酸盐、癸基甲基萘磺酸盐、十二烷基甲基萘磺酸盐、十四烷基甲基萘磺酸盐进行分析,通过液相色谱分离条件的优化,找到了最佳分析条件。

A brief review of preparation of three 1,1'binaphthyls with nonidentical groups in 2, 2'positions: 2amino2'hydroxy1,1'binaphthyl, 2hydroxy2'mercapto1,1'binaphthyl and 2amino2' mercapto1,1'binaphthyl was prespented, and the progress on their application in the asymmetrical synthesis was outlined.

概述了 2 ,2'位置上带有不同取代基的 1,1'联萘化合物,如 2氨基 2'羟基 1,1'联萘、2羟基 2'巯基 1,1'联萘和 2氨基 2'巯基 1,1'联萘的制备及在不对称合成中的应用研究进展。

Eight novel N,N′-naphthalene acyl substituted aromatic acylamino thiocarbamide s(Ⅱ1~Ⅱ8) were synthesized from aryl acylhydrazine and α-naphthalene acyl isothiocyanate, which was obtained by the reaction of potassium thiocyanate with α-naphthalene acyl chloride obtained from 2-naphthylacetic acid and thionyl chloride in anhydrous benzene.

通过α-萘乙酸和SOCl2在无水苯中反应制得α-萘乙酰氯,与硫氰酸钾反应生成α-萘乙酰基异硫氰酸酯,再与芳基酰肼进行加成反应,合成8种新型N,N′-萘乙酰基取代芳乙酰胺基硫脲类化合物(Ⅱ1~Ⅱ8)。

Eight novel N,N′-naphthalene acyl substituted aromatic acylamino thiocarbamides(Ⅱ1~Ⅱ8) were synthesized from aryl acylhydrazine and α-naphthalene acyl isothiocyanate, which was obtained by the reaction of potassium thiocyanate with α-naphthalene acyl chloride obtained from 2-naphthylacetic acid and thionyl chloride in anhydrous benzene.

通过α-萘乙酸和SOCl2在无水苯中反应制得α-萘乙酰氯,与硫氰酸钾反应生成α-萘乙酰基异硫氰酸酯,再与芳基酰肼进行加成反应,合成8种新型N,N′-萘乙酰基取代芳乙酰胺基硫脲类化合物(Ⅱ1~Ⅱ8)。

Five Butenafine's analogues were designed and synthesized according to the structure-activity relationship and operating mechanism of benzylamine antimycotics.

根据苄胺类抗真菌化合物的构效关系、作用机理,设计合成了 5个布替萘芬类似物,N (2 氯 5 吡啶甲基) N 甲基 1 萘甲胺,N ,N 二(4 叔丁基苄基) 1 萘甲胺,N (4 叔丁基苄基) N (2 氯 5 吡啶甲基) 1 萘甲胺,N ,N 二苄基 4 叔丁基苯甲胺,N (2 氯 5 吡啶甲基) N 苄基 4 叔丁基苯甲胺。

Mol/L and calcinations temperature at 500?℃. The solid superacid can be used as catalyst two times in the alkylation of naphthalene, and the total composition of MIPN,DIPN, and TIPN in product is over 98%. When the consumpt...

在催化剂用量为 10 %、反应温度为 160℃、反应时间为 2 5h的条件下连续两次使用SO2 - 4 TiO2 超酸催化萘对丙烯的烷基化反应,产品中一异丙基萘、二异丙基萘、三异丙基萘的总含量大于 98%。

The analytical results have shown that p ro ducts mainly consisted of some monosubstituted, disubstituted and a few trisub stituted naphthalenes. Except the low activity of HZSM-5 catalyst, all other z eolite catalysts have higher activity. HY and Hβ catalytic activities were the highest, and their naphthalene conversions attained to 79.12 and 55.79 percent respectively, but their selectivities for 2-isopropylnaphthalene, 2,6-diisopropylnaphthalene(2,6-DIPN) and 2,7-diisopropylnaphthalene ( 2,7-DIPN) were too low. ZM catalysts had good activity and much better selecti vity, especially for ZM4-3, of which its 2,6-DIPN/2,7-DIPN ratio was 2.97. Th er efore, some zeolite catalysts are recommended for shape selective isopropylat ion of coal tar naphthalene.

研究结果表明,煤焦油萘异丙基化产物主要由一取代萘、二取代萘以及少量三取代萘组成;除HZSM-5活性较低以外,其它催化剂均有较高的反应活性,其中HY和Hβ反应活性最高,萘转化率分别达75.15%和55.96%,但β位产物的选择性较差;ZM类催化剂既有一定的活性,又有较高的β选择性,是萘择形异丙基化反应理想的备选催化剂。

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