1, 8-naphthalimide derivative as well as preparation method and application thereof
The invention discloses a 1, 8-naphthalimide derivative as well as a preparation method and application thereof. The preparation method comprises the following steps: taking 4-bromo-1, 8-anhydride naphthalene as an initial raw material, and carrying out nucleophilic substitution reaction on the init...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses a 1, 8-naphthalimide derivative as well as a preparation method and application thereof. The preparation method comprises the following steps: taking 4-bromo-1, 8-anhydride naphthalene as an initial raw material, and carrying out nucleophilic substitution reaction on the initial raw material and 5-substituted benzotriazole to obtain intermediates a-c; the intermediates a-c react with three different diamine compounds to form naphthalimide, and the target product 1a-3c shown in the formula (I) is obtained. Wherein R1 is hydrogen, fluorine or chlorine; r2 is a dimethylamino group, a diethanol amino group or a piperazinyl group. The cytotoxicity of different tumor cells of all target compounds is evaluated through a CCK-8 experimental technology, and the compound 3a with better activity is used for researching the action with a DNA sequence of a human B lymphocytic neoplasm-2 proto-oncogene (Bcl-2). The compound can well act on a guanine G-rich sequence of a human proto-oncogene Bcl-2Pu39 |
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