On the base of benzimidazole and benzofuran containing heterocyclic system, several derivatives with expected biological activity were synthesized. 2,3-diaminodibenzofuran was the primary substance. Adding various cyc...On the base of benzimidazole and benzofuran containing heterocyclic system, several derivatives with expected biological activity were synthesized. 2,3-diaminodibenzofuran was the primary substance. Adding various cyclic agents, 2-phenil was got, 2-（o-chlorophenil）, 2-（o-oxyphenil）, 2-chlorometyl- and 2-hydroximethyl-3H-benzo[b[furo（3,2-f] benzimidazoles. The aforementioned substances were characterized by IR and NMR spectroscopy.展开更多
On the base of benzo [b] furo benzotriazoles several derivatives with expected biological activity were synthesized by alkylation and Mannich reactions. In the alkylation of ethyl iodide benzo [b] furo benzotriazoles ...On the base of benzo [b] furo benzotriazoles several derivatives with expected biological activity were synthesized by alkylation and Mannich reactions. In the alkylation of ethyl iodide benzo [b] furo benzotriazoles received 1-ethyl-benzo [b] furo [3,2-g] benzotriazole and 3-ethyl-benzo [b] furo [2,3-f] benzotriazole. Aminometilirization Mannich reaction conditions with ＂the application as amino compound diethylamine, morpholine and piperazine of benzo [b] furo benzotriazoles were received （N, N-diethylaminomethyl）, CN-morpholinometil） and （N-piperazinometil）-derivatives.展开更多
An efficient and easy method for one-pot three-component synthesis of l,3-disubstituted-3H-benzo[f]chromenes by the condensation of naphtol,aromatic aldehyde derivatives and phenylacetylene in the presence of ferric h...An efficient and easy method for one-pot three-component synthesis of l,3-disubstituted-3H-benzo[f]chromenes by the condensation of naphtol,aromatic aldehyde derivatives and phenylacetylene in the presence of ferric hydrogensulfate[Fe（HSO4）3], has been described.The catalyst displayed high activity which afforded the corresponding 1,3-disubstituted-3H-benzo[f]chromenes in satisfying yields.Alkyl-substituted phenols were examined and the corresponding benzopyran derivatives were synthesized in moderate yields.Heterogeneous nature of the using catalyst made it reusable for further chemical reactions.展开更多
The title compound ethyl 2-（6-（1,3-dioxo-4,5,6,7-tetrahydro-lH-isoindol-2（3H）- yl）-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4（3H）-yl） butanoate 3 was synthesized by the reaction of ethyl 2-（6-amino-7-fluoro-3-ox...The title compound ethyl 2-（6-（1,3-dioxo-4,5,6,7-tetrahydro-lH-isoindol-2（3H）- yl）-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4（3H）-yl） butanoate 3 was synthesized by the reaction of ethyl 2-（6-amino-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4（3H）-yl） butanoate with 4,5,6,7- tetraydrophthalic anhydride, and its structure was determined by X-ray single-crystal diffraction. The crystal belongs to the monoclinic system, space group P2 1/n with a = 9.3469（2）, b = 16.7715（5）, c = 13.7153（4） A, β= 104.9680（10）°, μ = 0.107 mm^-1, Mr = 430.42, V= 2077.08（10） ,A3, Z= 4, Dc = 1.376 g/cm3, F（000） = 904, T= 296（2） K, R = 0.0508 and wR = 0.1478.展开更多
The crystal structure of the new title compound 2-ethoxy-3-n-butyl- benzofuro[2,3d]pyrimidin-4（3H）-one （C16H18N2O3, Mr = 286.32） has been prepared and determined by singlecrystal X-ray diffraction. The crystal is ...The crystal structure of the new title compound 2-ethoxy-3-n-butyl- benzofuro[2,3d]pyrimidin-4（3H）-one （C16H18N2O3, Mr = 286.32） has been prepared and determined by singlecrystal X-ray diffraction. The crystal is of monoclinic, space group P21/c with a = 13.7167（14）, b = 13.113（1）, c = 8.378（1） A, β = 98.992（2）^o, V = 1488.4（3） A^3, Z = 4, Dc = 1.278, F（000） = 608, μ = 0.089 mm^-1, MoKa radiation （2 = 0.71073）, R = 0.0498, wR = 0.1238 for 2336 observed reflections with I 〉 2σ（I）. X-ray diffraction analysis reveals that all ring atoms in the benzo[4, 5]furo [2,3-d] pyrimi- dinone moieties are almost coplanar.展开更多
CoO-CeO2 is reported as a highly efficient and green recyclable catalyst, for the multicomponent synthesis of 4H-benzo[b]pyran derivatives. The catalyst was synthesized by a co-precipitation method and characterized b...CoO-CeO2 is reported as a highly efficient and green recyclable catalyst, for the multicomponent synthesis of 4H-benzo[b]pyran derivatives. The catalyst was synthesized by a co-precipitation method and characterized by XRD, BET specific surface area, ESEM and EDS analysis. This synthetic method provides several advantages such as simple work-up procedures, minimal amount of waste generated, short reaction time, and high yields of products.展开更多
A fundamental aspect of cancer development is cancer cell proliferation.Seeking for chemical agents that can interfere with cancer cell growth has been of great interest over the years.In our study,we found that a ben...A fundamental aspect of cancer development is cancer cell proliferation.Seeking for chemical agents that can interfere with cancer cell growth has been of great interest over the years.In our study,we found that a benzoxazine derivative,(6-tert-butyl-3,4-dihydro-2Hbenzo[b][1,4]oxazin-3-yl)methanol(TBM),could inhibit cell growth and caused significant cell cycle arrest in pulmonary adenocarcinoma A549 and H460 cells with wild-type p53,while not affecting the cell cycle distribution in p53-deleted H1299 lung adenocarcinoma cells.Since P53 plays an important role in regulating cell cycle progression,we analyzed the protein level of p53 by Western blot,and detected a significant elevation of p53 level after TBM treatment in A549 and H460 cells.The data suggested that TBM might specifically inhibit the proliferation of p53 wild-type lung adenocarcinoma cells through a p53-dependent cell cycle control pathway.More interestingly,results indicated that TBM might serve as a useful tool for studying the molecular mechanisms of lung cancer cell growth and cell cycle control,especially for the biologic process regulated by P53.展开更多
文摘On the base of benzimidazole and benzofuran containing heterocyclic system, several derivatives with expected biological activity were synthesized. 2,3-diaminodibenzofuran was the primary substance. Adding various cyclic agents, 2-phenil was got, 2-（o-chlorophenil）, 2-（o-oxyphenil）, 2-chlorometyl- and 2-hydroximethyl-3H-benzo[b[furo（3,2-f] benzimidazoles. The aforementioned substances were characterized by IR and NMR spectroscopy.
文摘On the base of benzo [b] furo benzotriazoles several derivatives with expected biological activity were synthesized by alkylation and Mannich reactions. In the alkylation of ethyl iodide benzo [b] furo benzotriazoles received 1-ethyl-benzo [b] furo [3,2-g] benzotriazole and 3-ethyl-benzo [b] furo [2,3-f] benzotriazole. Aminometilirization Mannich reaction conditions with ＂the application as amino compound diethylamine, morpholine and piperazine of benzo [b] furo benzotriazoles were received （N, N-diethylaminomethyl）, CN-morpholinometil） and （N-piperazinometil）-derivatives.
文摘An efficient and easy method for one-pot three-component synthesis of l,3-disubstituted-3H-benzo[f]chromenes by the condensation of naphtol,aromatic aldehyde derivatives and phenylacetylene in the presence of ferric hydrogensulfate[Fe（HSO4）3], has been described.The catalyst displayed high activity which afforded the corresponding 1,3-disubstituted-3H-benzo[f]chromenes in satisfying yields.Alkyl-substituted phenols were examined and the corresponding benzopyran derivatives were synthesized in moderate yields.Heterogeneous nature of the using catalyst made it reusable for further chemical reactions.
基金Supported by the National Natural Science Foundation of China (20872033, 20575019)Natural Science Foundation of Hunan Province (07JJ1003)+1 种基金Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education of China) (KLCBTCMR2008-14)Scientific Research Fund of Science and Technology Department of Hunan Province (No. 2006GK3067)
文摘The title compound ethyl 2-（6-（1,3-dioxo-4,5,6,7-tetrahydro-lH-isoindol-2（3H）- yl）-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4（3H）-yl） butanoate 3 was synthesized by the reaction of ethyl 2-（6-amino-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4（3H）-yl） butanoate with 4,5,6,7- tetraydrophthalic anhydride, and its structure was determined by X-ray single-crystal diffraction. The crystal belongs to the monoclinic system, space group P2 1/n with a = 9.3469（2）, b = 16.7715（5）, c = 13.7153（4） A, β= 104.9680（10）°, μ = 0.107 mm^-1, Mr = 430.42, V= 2077.08（10） ,A3, Z= 4, Dc = 1.376 g/cm3, F（000） = 904, T= 296（2） K, R = 0.0508 and wR = 0.1478.
基金This work was supported by the Natural Science Foundation of Hubei Province (2006ABB016)National Natural Science Foundation of China (20672041) Key Project of Science and Technology of Ministry of Education of China (107082, 106116)
文摘The crystal structure of the new title compound 2-ethoxy-3-n-butyl- benzofuro[2,3d]pyrimidin-4（3H）-one （C16H18N2O3, Mr = 286.32） has been prepared and determined by singlecrystal X-ray diffraction. The crystal is of monoclinic, space group P21/c with a = 13.7167（14）, b = 13.113（1）, c = 8.378（1） A, β = 98.992（2）^o, V = 1488.4（3） A^3, Z = 4, Dc = 1.278, F（000） = 608, μ = 0.089 mm^-1, MoKa radiation （2 = 0.71073）, R = 0.0498, wR = 0.1238 for 2336 observed reflections with I 〉 2σ（I）. X-ray diffraction analysis reveals that all ring atoms in the benzo[4, 5]furo [2,3-d] pyrimi- dinone moieties are almost coplanar.
基金the Behbahan Khatam Alanbia University of Technology for the partial support of this work
文摘CoO-CeO2 is reported as a highly efficient and green recyclable catalyst, for the multicomponent synthesis of 4H-benzo[b]pyran derivatives. The catalyst was synthesized by a co-precipitation method and characterized by XRD, BET specific surface area, ESEM and EDS analysis. This synthetic method provides several advantages such as simple work-up procedures, minimal amount of waste generated, short reaction time, and high yields of products.
基金This study was supported by the National Natural Science Foundation of China(Grant No.90813022)by the Natural Science Foundation of Shandong Province(Nos.Z2008D04 and Z2008B10).
文摘A fundamental aspect of cancer development is cancer cell proliferation.Seeking for chemical agents that can interfere with cancer cell growth has been of great interest over the years.In our study,we found that a benzoxazine derivative,(6-tert-butyl-3,4-dihydro-2Hbenzo[b][1,4]oxazin-3-yl)methanol(TBM),could inhibit cell growth and caused significant cell cycle arrest in pulmonary adenocarcinoma A549 and H460 cells with wild-type p53,while not affecting the cell cycle distribution in p53-deleted H1299 lung adenocarcinoma cells.Since P53 plays an important role in regulating cell cycle progression,we analyzed the protein level of p53 by Western blot,and detected a significant elevation of p53 level after TBM treatment in A549 and H460 cells.The data suggested that TBM might specifically inhibit the proliferation of p53 wild-type lung adenocarcinoma cells through a p53-dependent cell cycle control pathway.More interestingly,results indicated that TBM might serve as a useful tool for studying the molecular mechanisms of lung cancer cell growth and cell cycle control,especially for the biologic process regulated by P53.
