Synthesis,Crystal Structure and Antitumor Activity of a Novel Zn(Ⅱ)Complex with 2-(Nicotinoyloxy)acetic Acid Ligand

A novel Zn（Ⅱ） complex, [ZnL2（H2O）4]·H2O（1, HL = 2-（nicotinoyloxy）acetic acid）, was synthesized using Zn（OAc）2·2H2O and 2-（nicotinoyloxy）acetic acid as raw materials. Its structure has been elucidated by elemental analysis, IR and single-crystal X-ray diffraction. The structural analysis revealed that complex 1 crystallizes in triclinic, space group P1 and the Zn（Ⅱ） atom is six-coordinated with two N atoms from two different 2-（nicotinoyloxy）acetate anion ligands and four O atoms from coordinated water molecules. Complex 1 forms a 3D network structure by O–H···O hydrogen bonds. The antitumor activities of 2-（nicotinoyloxy）acetic acid ligand and its Zn（Ⅱ） complex were evaluated against human lung adenocarcinoma A549 cells, human hepatoma SMMC-7721 cells and human colon carcinoma Wi Dr cells.

Synthesis,Structure,and Surface Photo-electric Properties of a New Zn(Ⅱ)Coordination Complex Constructed from 2-(1H-benzotriazol-1-yl)acetic Acid and 1,10-Phenanthroline Ligands

A new binuclear Zn^Ⅱ coordination complex,Zn2（bta）（phen）2（Cl）3（1,Hbta = 2-（1Hbenzotriazol-1-yl）acetic acid and phen = 1,10-phenanthroline）,has been synthesized and characterized by single-crystal X-ray diffraction,IR spectroscopy,elemental,and photoluminescent analysis.Complex 1 crystallizes in triclinic system,space group P1 with a = 9.3040（19）,b = 10.694（2）,c =16.841（3） A°,α = 101.18（3）,β = 105.77（3）,γ = 91.72（3）°,V= 1575.8（5） A°3,C（32）H（22）Zn2Cl3N7O2,Mr =773.66,Dc = 1.631 g/cm^3,Z = 2,F（000） = 780,μ = 1.820 mm^-1,the final R = 0.1238 and wR =0.1131.X-ray diffraction analyses indicate that 1 displays two crystallographic independent Zn^Ⅱmetal centers with a distorted tetragonal pyramidal（ZnN4O） and a tetrahedral（ZnNCl3） geometries,respectively.The phen serves as a common N,N＇-bidentate ligand,and the bta^- as a unique N,O-bridged ligand in 1.In the crystal,1 forms a stable 3D supramolecular architecture by trifurcated hydrogen bonding C-H…C1 interactions and C-H…π,π…π stacking.1 showed photo-electric conversion properties.

Synthesis of 2-(Benzodioxol-2-yl)acetic Acids as PPARδAgonists

A new series of compounds, 2-（benzodioxol-2-yl）acetic acids, have been synthesized. Their structures were confirmed by MS and 1H-NMR. The preliminary pharmacological screening showed that these compounds exhibited potent human PPARδ agonist activities.

Synthesis and Crystal Structure Analysis of 2-(3,5-Di-tert-butyl-2-hydroxyphenyl)-2-(3,4- dimethylphenyl) Acetic Acid Dimethylamine Salt

A new compound 2-（3,5-di-tert-butyl-2-hydroxyphenyl）-2-（3,4-dimethylphenyl） acetic acid dimethylamine salt （[NH2（CH3）2][C24H31O3]） was synthesized and structurally determined. It is of monoclinic system, space group P21/c with a = 14.731（2）, b = 10.1185（10）, c = 17.065（2） A^°, β = 98.293（10）° ,Z = 4, V = 2517.0（6）A^°^3, Dc = 1.091 g/cm^3, F（000） = 904 and Mr= 413.58. The dihedral angle defined by two benzene rings is 98.23°.

α-(1-萘氧基乙酰氧基)烃基膦酸酯的合成与植调活性

合成了10个标题化合物4a～j.所有目标化合物的结构均经元素分析、IR、HNMR和MS确证.生物试验结果表明,该类化合物具有一定的植物生长调节活性.

A Sensitive HPLC-MS/MS Analysis of Dencichine in Rat Plasma and Its Application to Pharmacokinetics

In order to quantitate dencichine in biological samples, a selective and sensitive method for the determination of dencichine in rat plasma based on high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was developed and validated. (l)-2-amino-3-(carboxymethylthio)propionic acid was used as the internal standard (I.S.). After a protein precipitation extraction with acetonitrile, dencichine and the I.S. were chromatographed on an Xterra MS-C18 column. The mobile phase was consisted of 20mmol/L ammonium acetate solution-acetonitrile (35:65, V/V) at a flow rate of 0.2 mL/min. The detection was performed on a triple quadrupole mass via electrospray ionization (ESI) source in the positive mode. The intra- and inter-day precision (relative standard deviation, R.S.D.) values of dencichine were below 6.7%. The extraction recoveries were up 85%. The lower limit of quantification was 20 ng/ml, which was sensitive enough to detect the analyte. The HPLC-MS/MS method was successfully applied to the pharmacokinetic study after an intravenous administration of dencichine in Sprague-Dawley (SD) rat.

Clinical Study on Treatment of Advanced Non-small Cell Lung Cancer by Arsenious Acid Combined with Tα-1 Thymus Peptide and Megestrol Acetate

Objective: To observe the therape utic effect of arsenious acid combined with Tα-1 thymus peptide and megestro l acetate on advanced non-small cell lung cancer.Methods: Nintey-two patients were divided randomly into the tr eated group( n =45) and the control group( n =47). The treated group were tr eated with arsenious acid combined with Tα-1 thymus peptide and megestrol ac etate, and the control group were treated with chemotherapy in the NP protocol .Results: (1) Therapeutic effect :In the 36 patients of the treated group, 2 were evaluated as CR, 8 as PR, 9 as MR, 8 as SD and 9 as PD, the CR+PR rate being 27.7% (10/36), while in the 40 patients of the control group, the co rresponding numbers were 3, 10, 11, 9, 7 and 32.5% (13/40). Comparison between t he CR+PR rate between the two groups showed insignificant difference ( P >0.05 ). (2)Clinical benefit rate: The positive rate of Karnofsky scores in the treate d group and the control group was 44.4% and 20.0% respectively; and the positive rate of body weight in the two groups was 33.3% and 12.5% respectively, the dif ference between the two groups was significant ( all P <0.05). (3)Changes of T- cell subsets and NK cell activity: CD4 and CD4/CD8 ratio after treatment i n the treated group increased significantly ( P <0.05), while in the control group, CD3, CD4, CD4/CD8 ratio and NK cell activity all lowered significantly ( P <0.01). Comparison between the two groups after treatment showed significa nt difference in CD4, CD4/CD8 ratio and NK cell activity, with those in the trea ted group all higher than those in the control group ( P <0.01). (4)Adeverse -reaction: No serious adverse reaction was found in both two groups. (5)Media n survival period:The treated group was 30 weeks and that in the control group w as 28.5 weeks, and the difference between the two groups was insignificant ( P >0.05).Conclusion: Arsenious acid combined with Tα-1 thymus peptide and megestrol acetate was a relatively effective scheme with low toxicity in tre ating advanced NSCLC.

一类新型植物生长调节剂（Ⅱ）──β－萘氧乙酸二甲基烃基硅甲酯的合成

报道了一类新型含硅植物生长调节剂的合成。以二甲基氯甲基烃基硅烷和β－萘氧乙酸钾为原料制得了四种β－萘氧乙酸二甲基烃基硅甲酯，收率在５０％以上。其化学结构均经红外光谱、核磁共振憎和元素分析予以证实。用β－萘氧乙酸二甲基苄基硅甲酯对四季桔的保花保果试验，座果率比对照试验（只用β－萘氧乙酸）相对增加１４．１％，说明这类化合物有较好的生理活性。