A kind of chloroethyl nitrosourea with anticancer activity and its synthesis method

An anticancer activity, sodium nitrite technology, applied in the direction of organic active ingredients, medical preparations containing active ingredients, organic chemistry, etc. The effect of improving targeting and improving drug resistance
CN104031047BActive Publication Date: 2016-03-09BEIJING UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
BEIJING UNIV OF TECH
Publication Date
2016-03-09

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Abstract

The invention relates to novel chloroethyl nitrosourea with anticancer activity and a synthesizing method thereof. The chloroethyl nitrosourea is a compound with a structure of the general formula (I), wherein n is an integer of 2 to 6. The chloroethyl nitrosourea can be used for treating gliomatosis cerebri, colon cancer and leukemia; compared with the existing nitrosourea-type anticancer medicine, the drug resistance is lower, the chemical therapy effect is better, the preparation method is simple in operation, the reaction yield is high, the toxicity is small, the cost is low, the method is suitable for the industrialized production, the development prospect is wide, and the application value is good.
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Description

technical field

[0001] The present invention relates to novel chloroethyl nitrosourea and its synthesis method, in particular to N-(2-chloroethyl)-N'-2-(O 6 -Benzyl-9-guaninyl)alkyl-N-nitrosoureas and methods for their synthesis. Background technique

[0002] The main treatments for solid tumors include radiotherapy, surgery, chemotherapy, and biological therapy, and anticancer drugs have become a rapidly developing frontier in recent years. Nitrosoureas have shown good anticancer activity in both animal experiments and clinical applications, so they are widely used in the treatment of brain tumors, malignant lymphomas, leukemias, gliomas, and melanomas. Studies have shown that the main target of the interaction between nitrosourea and biological macromolecules is the DNA base, which can modify the N and O positions on the DNA base, thereby causing damage such as single / double strand breaks, or inducing sister chromosomal single body exchange and chromosomal aberrations. ...

Claims

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