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Phthalimide compounds with antiangiogenic activity and purpose thereof

A phthalimide and anti-angiogenesis technology, applied in medical preparations containing active ingredients, organic active ingredients, organic chemistry, etc., can solve problems such as unsatisfactory product effects, and achieve high safety and systemic The effect of low toxicity

Inactive Publication Date: 2013-05-08
赵庆春
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Purpose of the invention: the present invention provides a phthalimide compound with anti-angiogenesis activity and its application, the purpose of which is to solve the problem that the previous methods or products in the aspect of inhibiting angiogenesis have unsatisfactory effects

Method used

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  • Phthalimide compounds with antiangiogenic activity and purpose thereof
  • Phthalimide compounds with antiangiogenic activity and purpose thereof
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Experimental program
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specific Embodiment approach

[0030] Detailed ways: The present invention is further described below:

[0031] The present invention provides a phthalimide compound with anti-angiogenic activity:

[0032] The compound is a compound represented by formula (I)

[0033] (1)

[0034] R 1 and R 2 The same can represent hydrogen atom, methyl, benzyl, C 1 -C 18 Acyl, tert-butyl, triphenylmethyl, methoxymethyl, dimethylsilyl, tetrahydropyran, tert-butyldisilyl, benzoyl groups;

[0035] R 3 Can represent an oxygen atom, two hydrogen atoms.

[0036] R 4 Can represent hydrogen atom methyl, C 1 -C 18 Alkyl, benzyl, C 1 -C 18 Acyl, tert-butyl, triphenylmethyl, methoxymethyl, benzoyl groups.

[0037] 2. The phthalimide compound with anti-angiogenic activity according to claim 1, characterized in that: the compound is any one of formula (1) - formula (9):

[0038] (2)

[0039] (3)

[0040] (4)

[0041] (5)

[0042] (6)

[0043] (7)

[0044] (8)

[0045] (9)

[0046] The synthetic...

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Abstract

The invention provides phthalimide compounds with an antiangiogenic activity, and the compound is as shown in a formula (I). According to the invention, the new phthalimide compounds 4,6-dihydroxyisoindol-1,3-dione and 4,6-dihydroxyisoindol-1-one isolated from traditional Chinese medicine peeled puffball fruiting body are subjected to a full synthesis and a derivative reaction at the same time, and seven new compounds are obtained. The compounds provided by the invention has no cytotoxic activity to human lung carcinoma A549 cells, can inhibit VEGF secretion level of the human lung carcinoma A549 cells, and thus can control growth of tumors through blocking or interfering signal transduction pathways of the VEGF / VEGFR. Pharmacological activity shows that the compound system provided by the invention is low in toxicity and high in security, and has important significance in inhibiting the growth of the tumors through an antiangiogenic mechanism.

Description

technical field [0001] The invention relates to a phthalimide compound with anti-angiogenesis activity and its application. Background technique [0002] Angiogenesis plays an important role in tumor growth and metastasis. The growth and maturation of new blood vessels is the result of a complex multi-factor and multi-signal transduction process, which involves many angiogenic factors such as vascular endothelial growth factor (vascular endothelial growth factor, VEGF), angiopoietin, etc. And factors that inhibit angiogenesis such as endostatin, tumstatin, soluble vascular endothelial growth factor receptor (sVEGFR) and so on. In general, these two types of factors are in balance. Tumors can promote the secretion of angiogenesis factors, the most important of which is VEGF. A large number of research results show that VEGF is overexpressed in many cancer tissues, including liver cancer, lung cancer, colon cancer, ovarian cancer, breast cancer and so on. VEGF and its rece...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/48C07D209/46A61K31/4035A61P35/00
Inventor 赵庆春
Owner 赵庆春
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