Compound with MEK (Mitogen-activated and Extracellular signal-regulated Kinase) inhibiting function as well as preparation method and application of compound

A compound and alkyl technology, applied in the field of compounds with MEK inhibitory function and their preparation, can solve the problems of low kinase selectivity, large toxic and side effects, and inability to produce specific effects, etc.
CN102964326AInactive Publication Date: 2013-03-13PEKING UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
PEKING UNIV
Publication Date
2013-03-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a compound with an MEK (Mitogen-activated and Extracellular signal-regulated Kinase) inhibiting function as well as a preparation method and application of the compound. The structure of the compound disclosed by the invention is as shown in a formula (I). The preparation method of the compound disclosed by the invention comprises the steps of forming a coumarin ring by adopting a Pechmann reaction mainly and carrying out structural modification of different sites. In the binding experiment of the compound disclosed by the invention and MEK, the binding activity is up to 54.57nM; the anti-proliferation effect IC50 (half maximal inhibitory concentration) value on the melanoma cell A375 is up to 1.23 micrometers; the anti-proliferation effect IC50 value on the colon cancer cell HT-29 is up to 2.13 micrometers; and the activity is higher than that of a positive control U0126. The novel structure type coumarins compound with the MEK inhibiting function shows good MEK binding activity, MEK inhibiting activity, ERK (Extracellular signal Regulated Kinase) pathway inhibiting activity, anti-tumor effect and antiviral effect and has broad application value. The formula (I) is as shown in the specification.
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Description

Technical field

[0001] The invention relates to a compound and a preparation method and application thereof, in particular to a compound with MEK inhibitory function and a preparation method and application thereof. Such compounds have obvious anti-tumor and anti-viral effects, so they may be used in the treatment of tumors and viral diseases. Background technique

[0002] Mitogen-activated protein kinase (MAPK) is an important protein kinase discovered in the mid-1980s and is an important core signaling pathway in cells. The MAPK pathway is mainly divided into four types of sub-families: extracellular signal-regulated kinase (ERK) pathway, JNK pathway, p38 pathway and ERK5 pathway. The ERK pathway is an important family of the MAPK pathway. It is mainly composed of three core protein kinases Raf, MEK (Mitogen-activated and Extracellular signal-regulated Kinase) and ERK, which are activated sequentially to form an accurate and efficient signal network pathway. Play an important...

Claims

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