Synthesis, Crystal Structure and Biological Evaluation of Acridine-1,2,3-triazole Derivatives

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A series of acridine-1,2,3-triazole derivatives were designed, synthesized and characterized by NMR. 1-(2-methylacridinyl)-4-(4-methyl phenyl)-1,2,3-triazole(4f), C_(23)H_(18)N_4, was structurally determined by single-crystal X-ray diffraction. It crystallizes in the triclinic system, space group P1 with a = 9.585(4), b = 9.684(4), c = 11.339(5) ?, β = 88.250(7)o, V = 925.3(6), Z = 2, D_c = 1.258 g/cm~3, F(000) = 368, μ = 0.077 mm~(-1), the final R = 0.0808 and wR = 0.2218 for 3386 observed reflections(I > 2σ(I)). X-ray analysis indicates that the acridine ring is almost vertical to triazole ring with the dihedral angle nearly to be 75°. The crystal packing of the compound is stabilized mainly by π-π interaction. The preliminary biological tests display that some of the title compounds possess a good anti-tumour activity against MGC-803 and T24. A series of acridine-1,2,3-triazole derivatives were designed, synthesized and characterized by NMR. 1- (2-methylacridinyl) -4- It crystallizes in the triclinic system, space group P1 with a = 9.585 (4), b = 9.684 (4), c = 11.339 (5), β = 88.250 (7) o, V = 925.3 (6), Z = 2 and Dc = 1.258 g / the final R = 0.0808 and wR = 0.2218 for 3386 observed reflections (I> 2σ (I)). X-ray analysis indicates that the acridine ring is almost vertical to the triazole ring with the dihedral angle nearly to be 75 °. The preliminary biological tests display that some of the title compounds possess a good anti-tumor activity against MGC-803 and T24.
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