Synthesis And Biological Activities Of Novel Heterocyclic Compounds Containing 1,2,3-Triazole

Based on the mechanism of antitumor agents that target DNA,three series of compounds were designed,synthesized and charactered by modifying the structures of the naphthalimide skeleton and acenaphthenequinone derivatives,which consist of flat and rigid structures..A series of 1,2,3-triazol-1,8-naphthalimide derivatives were designed and synthesized via "Click Chemistry".Their spectra properties,DNA intercalative,DNA photo-damaging and antitumor activities were evaluated.The scatchard binding constants between CT DNA with N1-N6 were monitored by fluorescence spectroscopy technique.The result showed that they could effectively intercalate into the CT DNA and the scatchard binding constants reached 10⁴-10⁵ M^-1,So they could be used as effective DNA-target molecules.The antitumor activities test of these compounds exhibited efficient activities against 7721 and BGC-823 cell lines,especially compound N2 with thiomorpholinyl substituent,the IC₅₀ value against 7721 cell was 0.478×10^-6 M.A series of Novel 1,2,3-triazol-acenaphtho-fused heterocyclic compounds were designed and synthesized via "Click Chemistry".Their spectra properties,DNA intercalative,DNA photo-damaging and antitumor activities were evaluated.DNA-binding abilities of the E1-E6 were investigated by UV-vis,CD spectroscopic techniques and viscosity measurement,The results indicated that the compounds binded to DNA partly via intercalation,accompanied by kind of aggregation.DNA photo-damaging assayes showed that these compounds could effectively cleave supercoiled DNA,especially compound E2 with two cyanogen groups, which was in accordance with its excellent antitumor activity.Two novel 1,2,3-triazol-1,8-naphthalimide fluorophores were designed and synthesized via "Click Chemistry".Cell uptake experiments with fluorescence images indicated that V1 and V2 could be used for bioimaging in living cells,which implied the potentials of the fluorescence dyes V1 and V2 used as fluorescence agents.