Naphthalene ring-amido pyrimidine type compound and preparation method and application thereof

An aminopyrimidine and compound technology, applied in the field of compound preparation, can solve problems such as high toxicity, difficult source, drug resistance, etc., and achieve the effects of short synthesis route, simple preparation method and low requirement for experimental equipment
CN111138370AActive Publication Date: 2020-05-12GUIZHOU MEDICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
GUIZHOU MEDICAL UNIV
Publication Date
2020-05-12

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Abstract

The invention discloses a naphthalene ring-aminopyrimidine type compound as well as a preparation method and application thereof, and belongs to the technical field of preparation of new drug compounds. The preparation method disclosed by the invention comprises the following steps: carrying out an acylation reaction between 1-methoxynaphthalene and substituted phenylacetic acid to prepare 1-(4-methoxynaphthalene-1-yl)-2-substituted phenylethane-1-one; carrying out a reaction between 1-(4-methoxynaphthalene-1-yl)-2-substituted phenylethane-1-one and DMF-DMA to prepare (E)-3-(dimethylamino)-1-(4-methoxynaphthalene-1-yl)-2-substituted phenylpropyl-2-ene-1-one, and finally performing a ring closing reaction with guanidine hydrochloride and potassium carbonate to obtain the naphthalene ring-aminopyrimidine compound as shown in the general formular (I) in the specification. The naphthalene ring-amidopyrimidine compound disclosed by the invention has good activity of inhibiting tubulin polymerization, can effectively inhibit the proliferation activity of human breast cancer MCF-7 cells, can be used as a novel lead compound for antitumor drug research, and is suitable for market popularization and application.
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Description

technical field

[0001] The invention belongs to the technical field of compound preparation, and in particular relates to a naphthalene ring-aminopyrimidine type compound, a preparation method thereof and an application in preparation of tubulin inhibitor antitumor drugs. Background technique

[0002] Microtubules are composed of α and β tubulin dimers and are key components of the eukaryotic cytoskeleton. Microtubules are involved in a variety of cellular functions such as maintenance of cell shape, cell signaling, secretion, intracellular transport, and cell division. During mitosis in eukaryotic cells, microtubules form a spindle that guides chromosome division into two daughter cells. Disruption of microtubule function can cause dividing cells to arrest in the G2 / M phase, leading to apoptosis. Tubulin has become one of the important targets in the current research and development of anticancer drugs. Although paclitaxel, vinblastine and other tubulin inhibitor antineo...

Claims

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