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Halogenated diaryl acetylene analogue, its pharmaceutical composition and its preparation method and application

A technology of diaryl acetylene and halogenated diaryl, which is applied in the direction of drug combination, preparation of amino compounds from amines, and pharmaceutical formulations. It can solve problems affecting stability, inconvenient drug metabolism and pharmacokinetics, and achieve structural Stable, easy to handle and store, easy to effect in pharmaceutical research

Active Publication Date: 2017-01-04
UNIV OF KENTUCKY RES FOUND
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

As a drug, it affects its stability, and it is not convenient for research on drug metabolism and pharmacokinetics.

Method used

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  • Halogenated diaryl acetylene analogue, its pharmaceutical composition and its preparation method and application
  • Halogenated diaryl acetylene analogue, its pharmaceutical composition and its preparation method and application
  • Halogenated diaryl acetylene analogue, its pharmaceutical composition and its preparation method and application

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Embodiment Construction

[0026] In the process of developing new anticancer drugs, the inventors analyzed: Since SAM is the main donor of DNA methylation and protein methylation that regulate gene expression and tumor growth, it is generally believed that SAM synthesized by MAT2A can control key histones Modification, thereby controlling gene expression; then, the synthesis of a compound that blocks this process can provide a new idea for the development of anticancer drugs, that is, S-adenosyltransferase inhibitors can be used in cells to block Wnt Signaling and / or other pathways to inhibit the growth of cancer cells. Based on this, the inventors confirmed that some compounds can specifically inhibit methionine adenosyltransferase 2A (MAT2A) and reduce cellular S-adenosyl-methionine (SAM).

[0027] The present invention provides a kind of halogenated diaryl acetylene analogs including compounds of formula I and pharmaceutically acceptable salts thereof, wherein X 1 -X 5 is independently H, lower al...

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Abstract

The invention discloses a halogenated diaryl acetylene analog, whose chemical structural formula is shown in formula I: wherein X1-X5 is independently selected from one or more of H, lower alkyl or halogen, and at least one halogen; Y1-Y5 is independently selected from one or more of H, lower alkyl or NR1R2, and at least one NR1R2, wherein R1 and R2 are selected from H or lower alkyl. It also discloses its preparation method and its application for preparing medicine for treating cancer.

Description

technical field [0001] The invention belongs to a new compound in the field of medicine, its preparation method and application, and specifically relates to a new halogenated diarylethyne derivative, and also discloses its preparation method and its application for preparing cancer treatment drugs. Background technique [0002] Recently we found that a halogenated stilbene analog (stilbene analog: stilbene analog, such as compound 1) can inhibit Wnt target genes (such as the proto-oncogene c-Myc), and in vitro and in vivo experiments also demonstrated that these similar Drugs can inhibit the growth of intestinal cancer cells (see literature, Zhang et al., J Med Chem 2011, 54, 1288-97; ACS Chem Biol 2013: 8(4): 796-803 ; United States (U.S.) 8,664,276). However, such compounds suffer from the problem of cis / trans isomerism. We found that the trans structure has a higher [0003] [0004] anticancer activity. However, under conditions such as light, the cis structure ca...

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Application Information

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IPC IPC(8): C07C211/52C07C209/68A61K31/136A61P35/00
CPCA61K31/136A61P35/00
Inventor 大卫 S.瓦特刘春明维塔利 M.斯维里帕张文
Owner UNIV OF KENTUCKY RES FOUND