Quinoxalinone derivative with matrix metalloproteinase inhibitory activity and preparation method and application thereof

A technology of protease inhibition and quinoxalinone, applied in the direction of organic active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve inappropriate problems
CN101704792AInactive Publication Date: 2010-05-12SHANDONG UNIV
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Patent Information

Authority / Receiving Office
CN ยท China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG UNIV
Publication Date
2010-05-12
Estimated Expiration
Not applicable ยท inactive patent

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Abstract

The invention discloses a quinoxalinone derivative with matrix metalloproteinase inhibitory activity and a preparation method and an application thereof, belonging to the technical field of pharmaceutical chemistry. The derivative has the structure shown in the general formula (I), wherein the meanings of R1, R2, R3, R4, R5 and R6 are shown in the patent specification. The compound of the invention is proven to have specific MMP-2 inhibitory activity in the in vitro enzyme inhibitory activity experiments and to be an effective matrix metalloproteinase inhibitor so that the quinoxalinone derivative is expected to be developed to be a new anti-cancer drug.
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Description

technical field

[0001] The invention relates to quinoxalinone derivatives capable of inhibiting matrix metalloproteinases, a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. Background technique

[0002] Malignant tumors are one of the main diseases causing human death, and it is imminent to find highly selective anticancer drugs with high efficiency and low toxicity. Matrix metalloproteinases (Matrix metalloproteinases, MMPs) are a class of endopeptidases whose activity depends on zinc ions. Their main physiological function is to degrade and rebuild the extracellular matrix. Plays a key role in blood vessel growth. At present, 28 mammalian MMP subtypes have been discovered, so many MMPs family members are classified, and because the high expression of MMPs participates in many physiological processes of the human body, it is obviously inappropriate to inhibit all MMPs family members. People thus realize the importance...

Claims

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