1'-thio-aza indirubin compound, application and preparation method thereof

A technology of indirubin and compounds, which is applied in the field of medicine, can solve the problems that the anti-tumor effect of indirubin compounds has not been investigated, and achieve the effect of inhibiting or killing tumor cells
CN101747339AInactive Publication Date: 2010-06-23SHANGHAI JIAO TONG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI JIAO TONG UNIV
Publication Date
2010-06-23
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a 1'-thio-aza indirubin compound, application and a preparation method thereof, belonging to the field of medical technology. The preparation method of the compound comprises the steps of: respectively condensing 5-substituted, 6-substituted, 7-substituted isatin derivatives or 1-alkyl-7-azaindole-2,3-dione with thieno-(2,3-b)-pyridine-3-ketone or benzo-3(2H)-ketone to obtain a 1'-thio-aza indirubin compound in which R=O, wherein sodium carbonate is used as a catalyst; and reacting the 1'-thio-aza indirubin compound in which R=O with hydroxylamine to obtain a 1'-thio-aza indirubin compound in which R=NOH. The invention also relates to the application of the compound in the preparation of antineoplastic agents, acceptable salts in pharmacy synthesized by the compound with inorganic acid, organic acid or amino acid. The compound of the invention can suppress or kill tumor cells, have the character of anti-tumor activity and can be used for preparing medicines for treating tumors.
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Description

technical field

[0001] The invention relates to a compound in the technical field of medicine, its use and its preparation method, in particular to a 1'-thioazaidirubin compound, its use and its preparation method. Background technique

[0002] Indirubin is clinically used to treat chronic myelogenous leukemia, but its solubility is poor, and it will cause side effects on the gastrointestinal tract. During clinical application, some patients have to stop taking the drug because of this.

[0003] Find through literature search to prior art, Polychronopoulos, P. etc. published in " Journal of Medicinal Chemistry " (Journal of Medicinal Chemistry) 2004 the 47th phase 935~946 pages entitled " Structural basis for the synthesis of indirubins as potent and Selective inhibitors of glycogensynthase kinase-3 and cyclin-dependent kinases" (Structural basis of indirubin derivatives effectively selectively inhibiting glycogen synthesis kinase-3 and cyclin-dependent kinases), commented i...

Claims

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