Pyrimidotriazole-containing LSD1 inhibitor, preparation method and application

A technology of triazole and inhibitor, applied in the field of medicinal chemistry
CN106928235AInactive Publication Date: 2017-07-07ZHENGZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHENGZHOU UNIV
Publication Date
2017-07-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the field of medicinal chemistry, and discloses a class of pyrimidotriazole compounds, a preparation method thereof and the use of lysine-specific demethylase (hereinafter referred to as LSD1) as a target in the preparation of antitumor drugs Applications. The general formula of the compound of the present invention is shown in I. The LSD1 enzyme inhibitory activity experiment in vitro proves that this type of compound has obvious inhibitory and killing effects on a variety of tumor cells by inhibiting the activity of LSD1, and can be used as a lead compound for further development and applied to the preparation of anti-tumor drugs.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, and specifically relates to pyrimidotriazole compounds, their preparation methods and their use in antitumor drugs targeting histone lysine specific demethylase (hereinafter referred to as LSD1) application. Background technique

[0002] Tumor is a disease that seriously endangers human health and is difficult to overcome. There are many anti-tumor drugs that have been marketed, but there are still some problems in these drugs, such as high toxicity, weak targeting, and easy drug resistance. Therefore, the research and development of new anticancer drugs is particularly important.

[0003] Histone covalent modification is an important epigenetic mode, including histone acetylation, methylation, phosphorylation, and ubiquitination, among which acetylation and methylation are more frequently studied for the mechanism of histone modification. histone modification. Before 2004, histone methylati...

Claims

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