A new series of quinoxalinophenazine derivatives were synthesized in good yields by the reaction of 2,3-dibromonaphthalene-1,4-dione with different aryl-1,2-diamines in DMF as solvent at 120-130℃ or under reflux cond...A new series of quinoxalinophenazine derivatives were synthesized in good yields by the reaction of 2,3-dibromonaphthalene-1,4-dione with different aryl-1,2-diamines in DMF as solvent at 120-130℃ or under reflux conditions. 3,12-dimethylbenzo[a]quinoxalino[2,3-c] phenazine with bidentate character reacts with mercury(II) bromide to give suitable crystals. All products were confirmed by IR, ^1H and ^13C NMR, and the metal complex by single-crystal X-ray method. The crystal(C24H16Br2HgN4, Mr = 720.82) belongs to the triclinic system, space group P1 with a = 10.186(6), b = 10.421(6), c = 11.470(7) A, α = 98.670(7), β = 95.069(7), γ = 109.831(7)°, V = 1119.4(12) A3, Z = 2, Dc = 2.139 Mg/m^3, μ = 10.46 mm^-1, F(000) = 676, R = 0.043 and wR = 0.115 for 3982 observed reflections with I 〉 2σ(I).展开更多
Two new a-aminophosphonate derivatives containing thieno[2,3-d]pyrimidine, diethyl(((6-ethyl-2-methyl-4-oxothieno[2,3-d]pyrimidin-3 (4H)-yl)amino)(4-methoxyphenyl)methyl) phosphonate (1) and diethyl((4-b...Two new a-aminophosphonate derivatives containing thieno[2,3-d]pyrimidine, diethyl(((6-ethyl-2-methyl-4-oxothieno[2,3-d]pyrimidin-3 (4H)-yl)amino)(4-methoxyphenyl)methyl) phosphonate (1) and diethyl((4-bromophenyl)((6-ethyl-2-methyl-4-oxothieno[2,3-d]pyrimidin-3 (4//)-yl)amino)methyl)phosphonate (2), have been synthesized by a facial phosphorylated reaction, and their structures were characterized by NMR, IR, HRMS and X-ray single-crystal diffraction. Compound 1 (C21H28N3O5PS, Mr = 465.49) belongs to the orthorhombic system, space group P212121, with a = 10.83653(16), b = 12.04906(19), c = 18.0061(3) A, V= 2351.06(6) A3, Z= 4, Dc= 1.315 g/cm3, p = 2.177 mm-1, F(000) = 984.0, the final R = 0.0389 and wR = 0.0985 for all data. Compound 2 (C20H25BrN304PS, Mr = 514.37) belongs to the orthorhombic system, space group P212121, with a = 10.9187(5), b = 11.9522(4), c = 17.7667(7) A, V= 2318.60(16) A3, Z = 4, Dc= 1.474 g/cm3,μ = 4.175 mm^-1, F(000) = 1056.0, the final R = 0.0367 and wR = 0.0946 for all data.展开更多
Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxi...Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells (EC109), human hepatocarcinoma cells (HepG2), human gastric carcinoma cells (MGC-803), respectively, by the MTT method. The evaluation results revealed that compounds fimb, 6mf, 6mg, 6rid and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6rag presented excellent inhibitory effect against HepG2 (91.2%) and MGC-803 (94.4%) cells.展开更多
文摘A new series of quinoxalinophenazine derivatives were synthesized in good yields by the reaction of 2,3-dibromonaphthalene-1,4-dione with different aryl-1,2-diamines in DMF as solvent at 120-130℃ or under reflux conditions. 3,12-dimethylbenzo[a]quinoxalino[2,3-c] phenazine with bidentate character reacts with mercury(II) bromide to give suitable crystals. All products were confirmed by IR, ^1H and ^13C NMR, and the metal complex by single-crystal X-ray method. The crystal(C24H16Br2HgN4, Mr = 720.82) belongs to the triclinic system, space group P1 with a = 10.186(6), b = 10.421(6), c = 11.470(7) A, α = 98.670(7), β = 95.069(7), γ = 109.831(7)°, V = 1119.4(12) A3, Z = 2, Dc = 2.139 Mg/m^3, μ = 10.46 mm^-1, F(000) = 676, R = 0.043 and wR = 0.115 for 3982 observed reflections with I 〉 2σ(I).
基金supported by the National Natural Science Foundation of China(Nos.21105091 and 21171149)
文摘Two new a-aminophosphonate derivatives containing thieno[2,3-d]pyrimidine, diethyl(((6-ethyl-2-methyl-4-oxothieno[2,3-d]pyrimidin-3 (4H)-yl)amino)(4-methoxyphenyl)methyl) phosphonate (1) and diethyl((4-bromophenyl)((6-ethyl-2-methyl-4-oxothieno[2,3-d]pyrimidin-3 (4//)-yl)amino)methyl)phosphonate (2), have been synthesized by a facial phosphorylated reaction, and their structures were characterized by NMR, IR, HRMS and X-ray single-crystal diffraction. Compound 1 (C21H28N3O5PS, Mr = 465.49) belongs to the orthorhombic system, space group P212121, with a = 10.83653(16), b = 12.04906(19), c = 18.0061(3) A, V= 2351.06(6) A3, Z= 4, Dc= 1.315 g/cm3, p = 2.177 mm-1, F(000) = 984.0, the final R = 0.0389 and wR = 0.0985 for all data. Compound 2 (C20H25BrN304PS, Mr = 514.37) belongs to the orthorhombic system, space group P212121, with a = 10.9187(5), b = 11.9522(4), c = 17.7667(7) A, V= 2318.60(16) A3, Z = 4, Dc= 1.474 g/cm3,μ = 4.175 mm^-1, F(000) = 1056.0, the final R = 0.0367 and wR = 0.0946 for all data.
基金supported by the National Natural Sciences Foundations of China (Nos.21171149,21105091)
文摘Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells (EC109), human hepatocarcinoma cells (HepG2), human gastric carcinoma cells (MGC-803), respectively, by the MTT method. The evaluation results revealed that compounds fimb, 6mf, 6mg, 6rid and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6rag presented excellent inhibitory effect against HepG2 (91.2%) and MGC-803 (94.4%) cells.