Through simplifying the complicated skeleton of the natural product gambogic acid, two series derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer ce...Through simplifying the complicated skeleton of the natural product gambogic acid, two series derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method. The results showed that appropriate introduction of prenyl group to the small molecular compounds could elevate their antitumor activities. The structure–activities relationship of synthesized compounds certified that the bridgecore in gambogic acid was very important for keeping its antitumor activities.展开更多
The mixed ligand coordination compound of copper with norfloxacin (NFLX) and 1, 10-phen has been synthesized and characterized by means of X-ray single crystal diffraction. The structure features of the coordination ...The mixed ligand coordination compound of copper with norfloxacin (NFLX) and 1, 10-phen has been synthesized and characterized by means of X-ray single crystal diffraction. The structure features of the coordination compound are described. Antibacterial activities of the coordination compound have been tested against different microorganisms. The antitumor activities of the coordination compound on leukemia HL-60 cell line and liver cancer BEL-7402 cell line have been measured, respectively. The results indicated that the coordination compound has strong inhibitory effect on HL-60 and BEL-7402 cell lines.展开更多
2-methoxy-6-oxo-1, 4, 2-diazaphosphorinane-2-oxide 8, phosphorus counterpart of 2, 6-dioxopiperazine, was synthesized as antitumor agent. The new phosphorus heterocycle compound 8 is the key intermediate in the synthe...2-methoxy-6-oxo-1, 4, 2-diazaphosphorinane-2-oxide 8, phosphorus counterpart of 2, 6-dioxopiperazine, was synthesized as antitumor agent. The new phosphorus heterocycle compound 8 is the key intermediate in the synthesis of phosphorus counterpart of bisdioxopiperazine.展开更多
<span style="font-family:Verdana;">To synthesize, characterize and evaluate the antitumor potential derived from ruthenium compounds was generated in this study, from the precursor K[RuCl</span>&...<span style="font-family:Verdana;">To synthesize, characterize and evaluate the antitumor potential derived from ruthenium compounds was generated in this study, from the precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] a route in a simple and reproducible synthesis for a novel compound of coordinating Ru</span><sup><span style="font-family:Verdana;">+3</span></sup><span style="font-family:Verdana;"> with bipy and L-trip. The spectroscopic characterization in the mi</span><span style="font-family:Verdana;">ddle infrared region (FTIR) shows the interactions between Ru-(L-trip), evidenced by the displacement of the carboxylate ion band for</span><span><span style="font-family:Verdana;"> higher energies, and also by the displacements of aliphatic amine bands, suggesting that bidentate coordination of the L-trip ligand occurred. Analysis of the results obtained with thermoanalytical techniques showed that the minimum formula of the compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)]1/2H</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">O. Evaluation of the</span></span><span><span style="font-family:Verdana;"> antitumor potential of precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] showed the toxic effects on MCF-7 cell line, but </span></span><span style="font-family:Verdana;">did not show selectivity and not reached PBMC cells to the same extent. The evaluation of the antitumor potential of the newly synthesized compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)], demonstrated that the insertion of an L-tryptophan molecule into the precursor coordination sphere made it selective when compared to PBMC cells, for MCF-7 type tumor cells.</span>展开更多
Four novel compounds containing two pyridazinone units attached to one benzene or pyridine ring, protected and deprotected 1,5-di[3（2H）-pyridazinon-6-yl]benzene and 2,6-di[3（2H）-pyridazinon-6-yl]pyridine were synt...Four novel compounds containing two pyridazinone units attached to one benzene or pyridine ring, protected and deprotected 1,5-di[3（2H）-pyridazinon-6-yl]benzene and 2,6-di[3（2H）-pyridazinon-6-yl]pyridine were synthesized in eight steps, which provided a useful method for the preparation of pyridazinone derivatives via the Stetter and cyclization reactions. Their structures were characterized by ^1H NMR, ^13C NMR, and HRMS.展开更多
The title compound has been synthesized in good yield in H2O/ethersystem by using 2--chloroselenobenzoyl chloride as the key intermediate. its structurewas characterized by elemental analysisi IR, IH NMR and X--ray di...The title compound has been synthesized in good yield in H2O/ethersystem by using 2--chloroselenobenzoyl chloride as the key intermediate. its structurewas characterized by elemental analysisi IR, IH NMR and X--ray diffraction analyses.Crystal data: C15H19NO3Se, M.r= 340. 28, hexagonal, P61, a= 8. 903(2), c= 34. 352(1)A, V=2358. I A3, Z=6, Dx=1. 438 g/cm3, λ(CuKa)=l. 5418 A, μ=33. 56cm--1, F (000) = 1044, final R = 0. 034 for 1396 observed reflections. Molecules incrystal form helieal chains with intermolecular Se...O distance of 2. 812(5) A as wellas intramolecular Se ...O distance of 3. 089 (5) A. Biological studies show that thiscompound is very active against human tumor cells, including HCT--8, Bel--7402,A432, HL--60 and K562.展开更多
The title compound 4-(5-(2,6-difluorophenyl)-1,3,4-oxadiazol-2-ylthio)-2-(trifluoromethyl)thieno[2,3-d]pyrimidine(C15H5F5N4OS2, Mr = 416.35) was designed and synthesized as antitumor agent, and its structure was deter...The title compound 4-(5-(2,6-difluorophenyl)-1,3,4-oxadiazol-2-ylthio)-2-(trifluoromethyl)thieno[2,3-d]pyrimidine(C15H5F5N4OS2, Mr = 416.35) was designed and synthesized as antitumor agent, and its structure was determined by 1H NMR, 13C NMR, MS, elemental analysis and single-crystal X-ray diffraction. The crystal belongs to monoclinic system, space group P21/c with a = 9.904(2), b = 10.057(2), c = 16.595(3) ?, β = 100.000(3)°, V = 1627.9(6) ?3, Z = 4, F(000) = 832, Dc = 1.699 g/cm3, μ = 0.395 mm-1, R = 0.0468 and wR = 0.1255 for 4726 independent reflections(Rint = 0.0336) and 2847 observed ones(I > 2σ(I)). The in vitro antitumor activity of the title compound was preliminarily evaluated by the standard MTT assay.展开更多
文摘Through simplifying the complicated skeleton of the natural product gambogic acid, two series derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method. The results showed that appropriate introduction of prenyl group to the small molecular compounds could elevate their antitumor activities. The structure–activities relationship of synthesized compounds certified that the bridgecore in gambogic acid was very important for keeping its antitumor activities.
基金funded by the National Natural Science Foundation of China(No.50073019)
文摘The mixed ligand coordination compound of copper with norfloxacin (NFLX) and 1, 10-phen has been synthesized and characterized by means of X-ray single crystal diffraction. The structure features of the coordination compound are described. Antibacterial activities of the coordination compound have been tested against different microorganisms. The antitumor activities of the coordination compound on leukemia HL-60 cell line and liver cancer BEL-7402 cell line have been measured, respectively. The results indicated that the coordination compound has strong inhibitory effect on HL-60 and BEL-7402 cell lines.
文摘2-methoxy-6-oxo-1, 4, 2-diazaphosphorinane-2-oxide 8, phosphorus counterpart of 2, 6-dioxopiperazine, was synthesized as antitumor agent. The new phosphorus heterocycle compound 8 is the key intermediate in the synthesis of phosphorus counterpart of bisdioxopiperazine.
文摘<span style="font-family:Verdana;">To synthesize, characterize and evaluate the antitumor potential derived from ruthenium compounds was generated in this study, from the precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] a route in a simple and reproducible synthesis for a novel compound of coordinating Ru</span><sup><span style="font-family:Verdana;">+3</span></sup><span style="font-family:Verdana;"> with bipy and L-trip. The spectroscopic characterization in the mi</span><span style="font-family:Verdana;">ddle infrared region (FTIR) shows the interactions between Ru-(L-trip), evidenced by the displacement of the carboxylate ion band for</span><span><span style="font-family:Verdana;"> higher energies, and also by the displacements of aliphatic amine bands, suggesting that bidentate coordination of the L-trip ligand occurred. Analysis of the results obtained with thermoanalytical techniques showed that the minimum formula of the compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)]1/2H</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">O. Evaluation of the</span></span><span><span style="font-family:Verdana;"> antitumor potential of precursor K[RuCl</span><sub><span style="font-family:Verdana;">4</span></sub><span style="font-family:Verdana;">(bipy)] showed the toxic effects on MCF-7 cell line, but </span></span><span style="font-family:Verdana;">did not show selectivity and not reached PBMC cells to the same extent. The evaluation of the antitumor potential of the newly synthesized compound, [RuCl</span><sub><span style="font-family:Verdana;">2</span></sub><span style="font-family:Verdana;">(bipy)(L-trip)], demonstrated that the insertion of an L-tryptophan molecule into the precursor coordination sphere made it selective when compared to PBMC cells, for MCF-7 type tumor cells.</span>
基金Support by the National Natural Science Foundation of China(No.20571063)
文摘Four novel compounds containing two pyridazinone units attached to one benzene or pyridine ring, protected and deprotected 1,5-di[3（2H）-pyridazinon-6-yl]benzene and 2,6-di[3（2H）-pyridazinon-6-yl]pyridine were synthesized in eight steps, which provided a useful method for the preparation of pyridazinone derivatives via the Stetter and cyclization reactions. Their structures were characterized by ^1H NMR, ^13C NMR, and HRMS.
文摘The title compound has been synthesized in good yield in H2O/ethersystem by using 2--chloroselenobenzoyl chloride as the key intermediate. its structurewas characterized by elemental analysisi IR, IH NMR and X--ray diffraction analyses.Crystal data: C15H19NO3Se, M.r= 340. 28, hexagonal, P61, a= 8. 903(2), c= 34. 352(1)A, V=2358. I A3, Z=6, Dx=1. 438 g/cm3, λ(CuKa)=l. 5418 A, μ=33. 56cm--1, F (000) = 1044, final R = 0. 034 for 1396 observed reflections. Molecules incrystal form helieal chains with intermolecular Se...O distance of 2. 812(5) A as wellas intramolecular Se ...O distance of 3. 089 (5) A. Biological studies show that thiscompound is very active against human tumor cells, including HCT--8, Bel--7402,A432, HL--60 and K562.
基金supported by the National Natural Science Foundation of China(No.21262012)
文摘The title compound 4-(5-(2,6-difluorophenyl)-1,3,4-oxadiazol-2-ylthio)-2-(trifluoromethyl)thieno[2,3-d]pyrimidine(C15H5F5N4OS2, Mr = 416.35) was designed and synthesized as antitumor agent, and its structure was determined by 1H NMR, 13C NMR, MS, elemental analysis and single-crystal X-ray diffraction. The crystal belongs to monoclinic system, space group P21/c with a = 9.904(2), b = 10.057(2), c = 16.595(3) ?, β = 100.000(3)°, V = 1627.9(6) ?3, Z = 4, F(000) = 832, Dc = 1.699 g/cm3, μ = 0.395 mm-1, R = 0.0468 and wR = 0.1255 for 4726 independent reflections(Rint = 0.0336) and 2847 observed ones(I > 2σ(I)). The in vitro antitumor activity of the title compound was preliminarily evaluated by the standard MTT assay.
