Synthesis of benzimidazole-containing naphthalimide derivatives and applications of benzimidazole-containing naphthalimide derivatives on cancer resistance

A technology of benzimidazole and naphthalimide, applied to medical preparations containing active ingredients, antineoplastic drugs, drug combinations, etc., to achieve good tumor inhibitory activity and cell selectivity
CN102206203BInactive Publication Date: 2013-06-19DALIAN UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
DALIAN UNIV OF TECH
Publication Date
2013-06-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to synthesis of benzimidazole-containing naphthalimide derivatives and applications of the benzimidazole-containing naphthalimide derivatives on cancer resistance, and belongs to the field of organic synthesis and pharmaceutical chemistry technology. The benzimidazole-containing naphthalimide derivatives are obtained through a method that a benzimidazole group is introduced into a fourth position of a naphthalene ring of naphthalimide. Experiments of proliferation inhibiting effects of the benzimidazole-containing naphthalimide derivatives on cancer cells adopt a microculture tetrozolium (MTT) reduction method and aim at MCF-7 human breast cancer cells, Hela human cervical cancer cells and PC12 rat adrenal medullary pheochromocytoma differentiated cells. Results of the experiments show that the benzimidazole-containing naphthalimide derivatives have the advantages of good inhibitory activity against cancer cells and good selectivity on cancer cells.
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Description

technical field

[0001] The invention relates to the synthesis of a 4-(1H-benzimidazole-2-y1)-1,8-naphthalimide compound and its application in tumor cells, belonging to the technical fields of organic synthesis and medicinal chemistry. Background technique

[0002] Naphthalimide is a good precursor of DNA intercalator, and it is a research hotspot in recent years. The most famous derivatives that have been used clinically are amonafide (N-(β-dimethylaminoethyl)-3-amino-1,8-naphthalimide) and mitonafide (N-(β-di Methylaminoethyl)-3-nitro-1,8-naphthalimide), but because of its neurotoxic side effects, it has not entered clinical phase III. In order to improve the toxic and side effects and enhance the antitumor activity, the active site of naphthalimide is modified to synthesize new naphthalimide derivatives. The foreign Brana research group has reported a series of imidazonaphthimide derivatives, and the inhibitory activity of these derivatives to human colon cancer cells (...

Claims

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