Preparation and anti-tumor application of anthraquinone sulfonyl spiro derivative
The invention discloses an anthraquinone sulfonyl spiro derivative, which is characterized in that 1, 4-dihydroxy anthraquinone is used as a raw material, two sulfonyl groups are connected to the 1, 4-positions of the 1, 4-dihydroxy anthraquinone, and a spiro HXN6 derivative is synthesized at the 1...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses an anthraquinone sulfonyl spiro derivative, which is characterized in that 1, 4-dihydroxy anthraquinone is used as a raw material, two sulfonyl groups are connected to the 1, 4-positions of the 1, 4-dihydroxy anthraquinone, and a spiro HXN6 derivative is synthesized at the 1 position through nucleophilic substitution reaction. An in-vitro anti-tumor activity experiment is carried out on the synthesized anthraquinone sulfonyl spiro derivative HXN6 through an MTS method, and the experiment result shows that the activity of the derivative HXN6 is higher than that of an anthraquinone mother nucleus, the derivative HXN6 shows excellent anti-tumor activity, and the derivative HXN6 has good anti-tumor activity on IC50lt of DU-145; according to the present invention, the sulfur atom alkyl chain and the spiro structure are introduced as the main pharmacophore, such that the fat solubility of the compound is substantially improved, and the biological activity is significantly improved; in additi |
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