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

100%

Zhu W.-Z., Hu R.-D., Lin Q.-Y., Wang X.-X., Zheng X.-L.

Open Chemistry

2009

vol. 7

issue 3

569-575

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

Synthesis, DNA interaction and antibacterial activities of La(III) and Gd(III) complexes of Schiff base derived from o-vanillin and lysine

86%

Cheng J.-P., Lin Q.-Y., Rui-Ding H., Zhu W.-Z., Li H.-Q., Wang D.-H.

Open Chemistry

2009

vol. 7

issue 1

105-110

Two novel complexes, [La(HL)(H2O)2NO3] · NO3 · H2O and [Gd(HL)(H2O)2NO3] · NO3 · H2O, where HL is a Schiff base derived from o-vanillin and lysine, have been synthesized and characterized by elemental analysis, conductivity measurements, IR, 1H NMR and thermogravimetric analyses (TGA). The Schiff base ligand behaves as a tetradentate, coordinating through azomethine nitrogen, phenolic oxygen and two carboxylic oxygen atoms. The interaction of these complexes with calf thymus DNA (CT-DNA) was also investigated by spectrometric titration and viscometric measurements. The faint hypochromism of the complexes in the absorption spectra, the remarkable reduction of fluorescence intensity of ethidium bromide (EB) bound DNA, together with a small decrease in the viscosity of the DNA suggest that a partial intercalation may be the preferred binding mode between these two complexes and DNA. The antibacterial activity testing revealed that the complexes and their precursor Schiff base show a weak to moderate activity against Bacillus subtilis, Staphylococcus aureus and Escherichia coli. [...]

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2 Open Chemistry

2 2009

2 Lin Q.-Y.

2 Zhu W.-Z.

1 Cheng J.-P.

1 Hu R.-D.

1 Li H.-Q.

1 Rui-Ding H.

1 Wang D.-H.

1 Wang X.-X.

1 Zheng X.-L.

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

Synthesis, DNA interaction and antibacterial activities of La(III) and Gd(III) complexes of Schiff base derived from o-vanillin and lysine