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Indolone derivatives having different positions substituted and application thereof

A kind of derivative, indolinone technology, applied in the new compound preparation method and application field, can solve problems such as toxic and side effects

Inactive Publication Date: 2014-11-05
TIANJIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] The current method of treating cancer is chemical drug therapy, many of which inhibit the growth of cancer cells by inhibiting DNA synthesis. These drugs not only have lethal effects on cancer cells, but also have the same killing effect on normal cells. toxic side effects

Method used

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  • Indolone derivatives having different positions substituted and application thereof
  • Indolone derivatives having different positions substituted and application thereof
  • Indolone derivatives having different positions substituted and application thereof

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Embodiment Construction

[0024] In order to understand the present invention, the following examples will further illustrate the present invention; the following examples are illustrative and not restrictive, and the scope of protection of the present invention cannot be limited by the following examples.

[0025] The anti-tumor drug of the compound of formula (I) of the present invention is designed to use indole dione as the parent ring, and the biological activity of the compound is improved by modifying the 1,5 position, and introducing halogen, alkyl, and aromatic ring at the 5 position. , Five-membered heterocycle, six-membered heterocycle to study the influence of space size, electronic effect and chain length on activity, introduce alkyl and different substituted benzyl groups at the 1 position to study the influence factors of the N-1 group ; Then, the above-mentioned modification was performed on the 1,4, 1,6, and 1,7 positions to study the effect of different positions on the anti-tumor activit...

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Abstract

The invention relates to indolone derivatives having different positions substituted and an application thereof, and particularly relates to preparation of the indolone derivatives having the different positions substituted and the application of the indolone derivatives in preparation of anti-tumor drugs, wherein in the structural formula, R1 is one of benzyl or alkyl compounds, R2 is one of hydrogen or halogen or aryl compounds, R3 is one of hydrogen or halogen or aryl or five-membered heterocyclic or six-membered heterocyclic compounds, R4 is one of hydrogen or halogen or aryl compounds, and R5 is one of hydrogen or halogen or aryl compounds. The indolone derivatives having the different positions substituted are synthesized for the first time, anti-tumor activity tests of the synthesized compounds aiming at human hepatoma cells (HepG2), human leukemia cells (K562) and human colon cancer cells (HT-29) are performed, and results show that IC50 of the derivatives is less than 10 [mu]M.

Description

Technical field [0001] The invention belongs to the preparation method and application field of new compounds, in particular to a different position substituted indolinone derivative and its application. Background technique [0002] The current method of cancer treatment is chemotherapy. Many of these drugs inhibit the growth of cancer cells by inhibiting DNA synthesis. These drugs not only kill cancer cells, but also have the same killing effect on normal cells. These drugs usually have great effects. Toxic side effects. Therefore, researching new anti-cancer pathways and finding anti-cancer drugs that are easy to synthesize, have low side effects, and have high drug resistance have become a hot spot in drug research today. [0003] Isatin, also known as 2,3-indolequinone, is an anti-tumor active ingredient of traditional Chinese medicine Indigo Naturalis. Various types of chemical reactions can occur at positions 1, 2, and 3 and on the benzene ring, which provides the synthesis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/38C07D409/04C07D401/04C07D209/40C07D491/113A61K31/404A61K31/4439A61K31/407A61P35/00A61P35/02
CPCC07D209/38C07D209/40C07D401/04C07D409/04C07D491/113
Inventor 郁彭韩开林樊振川滕玉鸥周瑶宋彬彬曲昕
Owner TIANJIN UNIV OF SCI & TECH
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