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

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;H;N;, 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;= 1.258 g/cm;, F（000） = 368, μ = 0.077 mm;, 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.