New application of oxypiperazine acidamide compound

A technology of oxopiperazine amides and compounds, which is applied in the new application field of inhibiting PLK1 activity, can solve the problems of predicting PLK1 inhibitors, raw material drug quality control is immature, and has no obvious regularity, and achieves less toxic and side effects and better efficacy Precise, easy-to-obtain results

CN105616414AActive Publication Date: 2016-06-01XIANGBEI WELMAN PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
Publication Date
2016-06-01

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Abstract

The invention relates to an application of an oxypiperazine acidamide compound in inhibiting PLK1 activity. The oxypiperazine acidamide compound is selected from a compound in the formula I, its isomer, hydrate or salt. The oxypiperazine acidamide compound has advantages of definite effect, little toxic or side effect and good safety in the aspect of inhibiting PLK1 activity. In comparison with an existing compound for inhibiting PLK1 activity, the oxypiperazine acidamide compound of the invention is a known and used compound, raw materials are easily available, synthesis technology is mature, impurity research is sufficient, and quality control is mature. Thus, the compound of the invention is more convenient and easily available.
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Description

technical field

[0001] The invention relates to a new application of an oxopiperazine amide compound, in particular to a new application of the compound for inhibiting PLK1 activity. Background technique

[0002] The oxopiperazine amides represented by formula I are a class of known antibacterial drugs. It has good antibacterial effect on a variety of Gram-negative bacteria, and also has antibacterial effect on many anaerobic bacteria.

[0003]

[0004] Some antibacterial drugs have been used as antineoplastic drugs for a long time. For example, mitomycin, doxorubicin, epirubicin, actinomycin D, bleomycin, pingyangmycin, pelomycin, daunorubicin, etc. CN1911236A also reported that tetracycline antibacterial drugs (such as doxycycline) have anti-tumor, anti-inflammation and effects on cell survival in addition to antibacterial effects.

[0005] However, other antibacterial drugs have not been reported to have anti-tumor effects.

[0006] Clinically, it is a common pract...

Examples

Embodiment 1

[0058] Example 1 Inhibitory effect of oxopiperazine amides on PLK1 kinase

[0059] 1. Test substance: compounds represented by formula II to formula VIII of the present invention, amoxicillin, cefuroxime, penicillin, sulbactam, clavulanic acid, their hydrates and salts, and related compositions, etc.

[0060] 2. Test method:

[0061] 1) Preparation of each group of analyte solutions: DMSO was dissolved in 20 nM HEPES aqueous solution to form a DMSO / HEPES solution with a concentration of 20%. The test substances were divided into groups (multiple control groups, individual groups, combined groups), and the test substances of each group were respectively taken and dissolved in 20% DMSO / HEPES to obtain the solutions of the test substances of each group for use. The grouping situation and the highest concentration of the analyte in each group of the analyte solution obtained (for the joint group, it refers to the concentration of the compound shown in formula II to formula VIII i...

Embodiment 2

[0076] Example 2 Inhibitory effect of oxopiperazine amides on tumors

[0077] Taking prostate cancer and ovarian cancer as examples below, the therapeutic effects of the oxopiperazine amides compounds of the present invention on cell proliferation diseases, especially tumors will be further illustrated.

[0078] 1. Treatment of the object to be tested:

[0079] Test substances: compounds represented by formula II to formula VIII in the present invention, amoxicillin, paclitaxel, sulbactam, their salts and hydrates, and related compositions, etc.

[0080] Solution preparation: divide the test substance into groups (multiple control groups, separate groups, combined groups), take the test substance in each group respectively, first add 1.23ml castor oil, shake well to dissolve, then add 1.23ml absolute ethanol , Shake well to dissolve, and prepare mother solutions of each group of analytes. Grouping situation and the concentration of the analyte in each group of analyte mother...