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Beta-carboline ruthenium compound as well as preparation method and application thereof

A complex, ruthenium carboline technology, applied in the field of β-carboline ruthenium complexes and their preparation of autophagy inducers as anti-tumor drugs, can solve the problems of autophagy-inducing gene Beclin1 loss, loss of tumor inhibitory effect, etc., to achieve Excellent effect

Inactive Publication Date: 2010-09-29
SUN YAT SEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in a variety of human tumors, the autophagy-inducing gene Beclin1 is deleted or mutated, thus losing its inhibitory effect on tumors

Method used

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  • Beta-carboline ruthenium compound as well as preparation method and application thereof
  • Beta-carboline ruthenium compound as well as preparation method and application thereof
  • Beta-carboline ruthenium compound as well as preparation method and application thereof

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Embodiment Construction

[0025] The β-carboline ruthenium complex of the present invention has a molecular formula of [Ru(N^N) 2 (Nh) X Cl Y ](A^A) z , wherein N^N is selected from bpy or phen; A^A is selected from PF 6 or SO 3 CF 3 ; X=1 or 2, Y=2-X, Z=1 or 2; The molecular structural formula of the cationic moiety corresponding to the complex is shown in A1, A2, A4, A5:

[0026]

[0027] The preparation method of above-mentioned complex, will cis-[Ru(bpy) 2 Cl 2 ]·2H 2 O or cis-[Ru(bpy) 2 Cl 2 ]·2H 2 O and 9H-pyridino[3,4-b]indole (Norharman) were dissolved in aqueous ethanol, refluxed, evaporated under reduced pressure, filtered to remove unreacted 9H-pyridino[3,4-b]indole ligand, added NH 4 PF 6 , after the product is separated out, it is washed and then vacuum-dried, purified and recrystallized to obtain [Ru(bpy) 2 (Nh)Cl](PF 6 ) or [Ru(phen) 2 (Nh)Cl](PF6 ); or, put cis-[Ru(bpy) 2 Cl 2 ]·2H 2 O or cis-[Ru(bpy) 2 Cl 2 ]·2H 2 O and AgSO 3 CF 3 After the reaction, AgCl was...

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Abstract

The invention discloses a beta-carboline ruthenium compound. The molecular formula of the beta-carboline ruthenium compound is [Ru (N^N) 2 (Nh) XClY] (A^A)z, wherein N^N is selected from bpy or phen; A^A is selected from PF6 or SO3CF3; X is equal to 1 or 2, Y is equal to 2-X, and Z is equal to 1 or 2; or the molecular formula of the beta-carboline ruthenium compound is [Ru (N^N) 2 (1-Py-betaC)] (PF^)2, wherein N^N is selected from bpy, phen or DIP. On a molecular mechanism, the invention proves that the beta-carboline ruthenium compound can be used for treating cancers and has a better effectthan the effects of that of the traditional metal compound cisplatin with wide application and ruthenium compounds NAMI-A in clinical tests; . Thethe beta-carboline ruthenium compound for treating the cancers as an autophagic cell inducer fills the blank of the prior art and develops a new line for developing a new generation of high-efficiency medicaments for treating malignant tumors.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a β-carboline ruthenium complex and its use for preparing an autophagy inducer as an antitumor drug. technical background [0002] 1. Introduction to β-carboline ruthenium complexes [0003] In recent years, the development of metal complexes with biologically active molecules as ligands has provided a broader space for the design of new drugs for high efficiency and targeted activity. Studies of such complexes reveal that the combination of intrinsic properties of metals and bioactive ligand molecules provides clues to the possibility of overcoming current drug resistance pathways. [0004] β-carboline alkaloids are a class of synthetic and natural compounds with broad-spectrum biopharmacological activities including sedative, anxiolytic, hypnotic, anticonvulsant, antitumor, antiviral, antiparasitic and antibacterial. (Cao, Peng et al. 2007) It has been reported that β-carbo...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00A61K31/444A61K31/437A61K31/4745
Inventor 徐安龙彭文烈谭彩萍王旻谞朱一平吴寿海赖森森连武
Owner SUN YAT SEN UNIV
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