Synthesis, DNA-binding and antiproliferative activity of N-(Nitrogen heterocyclic) norcantharidin acylamide acid

作者: Wen-Zhong Zhu , Rui-Ding Hu , Qiu-Yue Lin , Xiao-Xia Wang , Xiao-Liang Zheng

DOI: 10.2478/S11532-009-0058-3

关键词:

摘要: Two novel norcantharidin acylamide acids (HL1=N-pyrimidine acid, C12H13N3O4; HL2=N-pyridine C13H14N2O4) were synthesized by a reaction of norcantharidin(NCTD) with 2-aminopyrimidine and 2-aminopyridine, respectively. Their structures characterized elemental analysis, IR, UV 1 H NMR. Fluorescence titration viscosity measurements indicated that HL1, HL2 HL3 (HL3=N-phenyl C14H15NO4) can bind calf thymus DNA via partial intercalation. The liner Stern-Volmer quenching constant Ksv values for 2.05 × 104 L mol−1, 1.15 mol−1 8.30×103 compounds containing heterocycle HL1 have been found to cleave pBR322 plasmid at physiological pH temperature. test antiproliferation activity showed the had moderate strong antiproliferative ability against tested cell lines except SMMC7721 line. results attached was favorable activity. This result consistent binding experiment.

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