A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroac...A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroacetamido）anthraquinones. Their cytotoxic activities against HeLa and MCF-7 ceils were preliminarily evaluated and compound 9a with mono-azasugar pendant at 2-position showed similar activity to the control drug （Cisplatin）.展开更多
A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against He/a...A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against He/a, A549 and K562 cells, which showed that the length of the side chains of the amino acids influenced the cytotoxic activities. Moreover, compound 7d showed a very good cytotoxic activity against A549 cells with an IC50 value of 4.78 μmol L-1, Furthermore, the UV-vis, fluorescence, and circular dichroism （CD） spectroscopies and thermal denaturation experiment indicated that compounds 6a, 6d and 7a, 7d, as DNA intercalators, exhibited binding affinities with calf-thymus DNA （Ct-DNA）.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21372059 and 21172051)the Hebei Key Basic Research(No.12966417D)+1 种基金the Hebei Natural Science Foundation(No.B2012201041)the Foundation of Hebei Education Department(No.YQ2013006)
文摘A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroacetamido）anthraquinones. Their cytotoxic activities against HeLa and MCF-7 ceils were preliminarily evaluated and compound 9a with mono-azasugar pendant at 2-position showed similar activity to the control drug （Cisplatin）.
基金supported by the National Natural Science Foundation of China(Nos.21372059 and 21172051)the Hebei Natural Science Foundation(No.B2012201041)the Foundation of Hebei Education Department(No.YQ2013006)
文摘A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against He/a, A549 and K562 cells, which showed that the length of the side chains of the amino acids influenced the cytotoxic activities. Moreover, compound 7d showed a very good cytotoxic activity against A549 cells with an IC50 value of 4.78 μmol L-1, Furthermore, the UV-vis, fluorescence, and circular dichroism （CD） spectroscopies and thermal denaturation experiment indicated that compounds 6a, 6d and 7a, 7d, as DNA intercalators, exhibited binding affinities with calf-thymus DNA （Ct-DNA）.
