Synthesis and acaricidal activity of strobilurin-pyrimidine derivatives简

Pyriminostrobin, a new acaricide, was discovered in our previous studies. Because introducing fluorine into organic compounds can increase bioactivity, pyriminostrobin was modified as a series of strobilurin-pyrimidine derivatives for biological screening. The compounds were characterized by 1H NMR, MS and elemental analysis. Preliminary bioassays demonstrated that compounds 7e and 7i exhibited significant control against Tetranychus cinnabarinus （Boisd.） at 0.625 mg L^-1, and their acaricidal potencies were higher than pyriminostrobin in a greenhouse. The relationship between structure and acaricidal activity was also studied.     

Design of novel bis-benzimidazole derivatives as DNA minor groove binding agents

A new series of bis-benzimidazole derivatives were designed and synthesized.In vitro cytotoxicity evaluation showed that these compounds exhibited high activity against the selected tumor cells.Among them,compound 9 owned the best potential,its IC_(50) values being 5.95 μmol/L(mononuclear tumor cell line(U937)) and 5.58 μmol/L(cervical cancer cell(HeLa)).Fluorescence and UV-vis studies showed that compound 9 could bind into the minor groove of DNA.     

A facile electrochemical method for the synthesis of new sulfonamide derivatives of potential biological significance

The electrochemical synthesis of some new sulfonamide derivatives was carried out via the electrochemical oxidation of 2,3-dihydrophthalazine-l,4-dione （1） in the presence of arylsulfinic acids （2a and 2b） as nucleophiles. The results show that, the electrogenerated phthalazine-l,4-dione （lox） participates in a Michael type addition reaction with 2a or 2b and via an EC mechanism to produce the corresponding sulfonamide derivatives. This method provides a one-pot procedure for the synthesis of new sulfonamide derivatives of potential biological significance in good yields without using toxic reagents at a carbon electrode in an environmentally friendly manner.     

Synthesis and in vitro cytotoxic activities of sorafenib derivatives

A series of novel sorafenib derivatives have been designed and synthesized.The cytotoxic activities of these compounds were tested in three tumor cell lines.Most of the compounds showed potent antiproliferative activity against the tested cell lines with IC50= 0–20 mmol/L.Some compounds demonstrated competitive antiproliferative activities to sorafenib against all three cancer cell lines.Among them,compound 5g demonstrated significant inhibitory activity against A549,ACHN and MDAMB-231 cell lines with IC50values of 1.29,1.99,3.11 mmol/L,respectively.     

Synthesis of novel,azasugar-modified anthraquinone derivatives and their cytotoxicity

A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroacetamido）anthraquinones. Their cytotoxic activities against HeLa and MCF-7 ceils were preliminarily evaluated and compound 9a with mono-azasugar pendant at 2-position showed similar activity to the control drug （Cisplatin）.     

N-Fluorinated phenyl-N＇-pyrimidyl urea derivatives： Synthesis,biological evaluation and 3D-QSAR study

With the increase of herbicide-resistant weeds, novel, more selective and even more potent herbicides to control weeds are needed. In this paper, a series of N-fluorinated phenyl-N＇-pyrimidyl urea derivatives were synthesized and screened for their herbicidal activities against Amaranthus retroflexus （AR） and Setaria viridis （ SV）. Compound 2S （N-（3-trifluoromethylphenyl）-N＇-（2-amino-4-chloro-6-methylpyr- imidyl） urea） exhibited marked herbicidal activity against SV（IC50 =11.67 mg/L） and is more potent than bensulfuron （IC50= 27.45 mg/L）, a commercially available herbicide. A statistically significant CoMFA model with high prediction abilities （q2 = 0.869, r2 = 0.989） was obtained.     

＂Amano＂ lipase DF-catalyzed efficient synthesis of 2,2＇-arylmethylene dicyclohexane-1,3-dione derivatives in anhydrous media

A simple and efficient method was developed for the synthesis of 2.2＇-arylmethylene dicyclohexane-1,3- dione derivatives via the Knoevenagel-Michael cascade reactions of aromatic aldehydes and 1,3-cyclic diketones catalyzed by ＂Amano＂ lipase DF, which expands the application field of enzyme catalytic promiscuity. This protocol provides several advantages over the traditional chemical synthesis, such as simple work-up procedure, high yields Cup to 94%） and environmental friendliness.     

Synthesis and thermal properties of novel calix[4]arene derivatives containing 1,2,3-triazole moiety via K2CO3-catalyzed 1,3-dipolar cycloaddition reaction

Two calix[4]arene derivatives containing 1,2,3-triazole moiety were synthesized via K2CO3-catalyzed1,3-dipolar cycloaddition reaction between calix[4]arene-based azide and active methylene compounds in good yields.The structures of the two compounds synthesized herein were fully confirmed by 1HNMR,,（13）C NMR,and MS（ESI）.The thermal analysis showed that the mass losses of the synthesized compounds 4 and 5 containing 1,2,3-triazole groups are similar to each other.     

具有聚集诱导发光特性的咔唑衍生物的合成及其理化性质研究

以咔唑、亚芴基肼等为原料,通过suzuki反应合成了2个新型咔唑衍生物:N-乙基-3,6-双(亚芴基肼基-5-亚甲基-2-噻吩)咔唑(S1)和N-(亚芴基肼基-4-亚甲基苯基)-3,6-双(亚芴基肼基-5-亚甲基-2-噻吩)咔唑(S2)。用FTIR、1HNMR、元素分析对S1和S2的结构进行表征,并考察其紫外吸收光谱、荧光光谱、电化学行为和热稳定性。结果表明:S1和S2薄膜的最大发射波长分别在637和649nm处,均发射红色荧光,且S1和S2均具有良好的聚集诱导发光(AIE)特性;S1和S2的HOMO能级分别是-5.26和-5.29e V,与正电极(ITO)的功函数(-4.8 e V)相匹配,可有效降低空穴注入能垒,有利于空穴的传输;S1和S2的热分解温度分别是351和360℃,均具有良好的热稳定性。     

6-氯-N,N-二甲基嘧啶-4-胺的晶体结构研究

X-射线单晶衍射结果表明,所合成的6-氯-N,N-二甲基嘧啶-4-胺的晶体结构属正交晶系,Pbca空间群,晶胞参数为a=10.922(2),b=7.386(3),c=17.861(6)。由于在其晶格内存在着潜在的C—H…N和C—H…Cl两类分子间弱相互作用力,形成了二维网络结构,化合物变得更加稳定。