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Rebeccamycin analogue with anticancer activity and synthesis method thereof

A technique for phathomycin and anticancer activity, which is applied in the field of phathomycin analogs with anticancer activity and the field of synthesis

Inactive Publication Date: 2013-03-27
HENAN NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

At present, although a large number of tritemycin analogs have been synthesized, they have not been used in clinical treatment because of the lack of ideal water solubility.

Method used

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  • Rebeccamycin analogue with anticancer activity and synthesis method thereof
  • Rebeccamycin analogue with anticancer activity and synthesis method thereof
  • Rebeccamycin analogue with anticancer activity and synthesis method thereof

Examples

Experimental program
Comparison scheme
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Embodiment Construction

[0027] 1. Synthesis of N-glycosyl phaeomycin analog I series compounds

[0028] We choose the following six glycosyl intermediates as examples to illustrate the synthesis of N-glycosyl phaeomycin analog I series compounds.

[0029]

[0030] Starting from various sugars and aminoethanol, we synthesized six kinds of glycosyl intermediates according to the following synthetic route, and chose the following glycosyl intermediates as an example to illustrate the synthesis of Phetalemycin analogues:

[0031]

[0032] 1) Synthesis of N-Phth aminoethanol

[0033] Add phthalic anhydride (1mol) into a 10mL round-bottomed flask, and then add aminoethanol (1eq) dropwise into the flask with stirring, and the reaction is exothermic. After the dropwise addition, the temperature was raised to 100° C. with an oil bath, and the reaction was completed after about 1 hour. The temperature of the solution was lowered to room temperature, and the solution became solid. Distilled water was a...

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Abstract

The invention relates to a rebeccamycin analogue with anticancer activity and a synthesis method thereof. Groups, such as glycosyl, amino acid, basic group, alkyl, and the like are introduced into the N-6 site to synthesize the rebeccamycin analogue, therefore, a method for obtaining the rebeccamycin analogue with more favorable biological activity and favorable water solubility is provided.

Description

technical field [0001] The invention relates to a class of compounds with anticancer activity, in particular to a novel compound of N-6 substituted phaemycin analogue with anticancer activity and a preparation method thereof. Background technique [0002] In 1985, Doyle et al discovered Rebeccamycin. It is a microbial metabolite isolated from the culture medium of actinomycete Saccharothrix Aerocoligenes, and its structure consists of indole[2,3-a]pyrrole[3,4-c]carbazole nucleus (abbreviated as indolecarbazole Nucleus) and β-glucose are composed of two major parts, as shown in the figure below. [0003] [0004] Studies have shown that phaeomycin is a new type of natural antibiotic, which has a certain inhibitory effect on topoisomerase I (Topoisomerase I) after camptothecin, and can induce the breakage of eukaryotic DNA to produce relatively Substances with strong antitumor activity. DNA binding experiments showed that when phaeomycin interacted with DNA, the indoloc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7056A61K31/7076A61K31/7068A61K31/7072A61K31/706C07H19/04C07H1/00A61P35/00
Inventor 张贵生王军强师君红刘小兵刘青锋毕晶晶
Owner HENAN NORMAL UNIV
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