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Fragrant geldanamycin derivative and its preparing method and use

A technique for geldanamycin and aromatization, which is applied in the field of aromatization of geldanamycin derivatives, and can solve problems such as benzoquinone reduction that have not yet been seen

Inactive Publication Date: 2007-08-08
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In terms of structure type, in all the geldanamycin compounds that have been recorded in the literature so far, it has not been seen that the benzoquinone of this type of compound is reduced to an aromatic ring and there is an oxygen heterocycle derivatization on the aromatic ring. thing

Method used

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  • Fragrant geldanamycin derivative and its preparing method and use
  • Fragrant geldanamycin derivative and its preparing method and use
  • Fragrant geldanamycin derivative and its preparing method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Fermentative production and separation and purification of embodiment 1 compound 1

[0095] Fermentation production

[0096] Toxin-producing bacteria

[0097] The toxin-producing bacteria used for fermentative production of compound 1 in this example was isolated from soil samples collected from Xishuangbanna and identified as Streptomycespseudoverticillus strain YN17707 CGMCC No.1452 through taxonomic studies.

[0098] Fermentation culture of toxin-producing bacteria

[0099] According to the conventional method of cultivating microorganisms, an appropriate amount of Streptomycespseudoverticillus YN17707 CGMCC No.1452 strain was taken, inoculated into an eggplant-shaped flask on the Gaoshi Synthetic No. 1 agar solid slant medium, and activated for 7 days in an incubator at 28 degrees Celsius. Get the eggplant-shaped bottle slope that has been activated and cultivated for 7 days, add 15 milliliters of sterile water, scrape off the spores with an inoculation needle, ma...

Embodiment 2

[0109] The separation and purification of embodiment 2 compound 2

[0110] Get 30 grams of the chloroform extract obtained in the above-mentioned Example 1, dissolve it with an appropriate amount of chloroform, add 50 grams of silica gel G (200-300 mesh) produced by Qingdao Ocean Chemical Factory to mix the sample, add to the silica gel that is equipped with 300 grams of thin-layer chromatography. 60H (Qingdao Haiyang Chemical Factory) glass decompression column, carry out decompression column chromatography, use chloroform-methanol system (100:0→80:20) gradient elution, every 500ml is a fraction, and several fractions are obtained. share. According to the results of TLC detection and activity test, the corresponding fractions were combined to obtain the active component Fr-4 containing compound 2 (the elution fraction of chloroform-methanol 80:20). Dissolve the active component Fr-4 in an appropriate amount of chloroform, add an appropriate amount of silica gel G (200-300 me...

Embodiment 3

[0118] Example 3 Cell Cycle Inhibitory Activity Test of Compound 1 and Compound 2

[0119] Experimental samples and experimental methods

[0120] Preparation of the tested sample solution

[0121] The test samples were the pure compound 1 and compound 2 separated and refined in the above-mentioned example 1 and example 2. Accurately weigh an appropriate amount of sample, and use methanol to make a solution of the required concentration for testing the activity.

[0122] Subculture of cell lines and cells

[0123]The activity test adopts the temperature-sensitive mouse breast cancer tsFT210 cell line, and the cells are subcultured in RPMI-1640 medium containing 10% FBs at 32 degrees Celsius in a cell incubator filled with 5% carbon dioxide.

[0124] Flow Cytometry Activity Assay Method

[0125] asynchronous culture test

[0126] Take the tsFT210 cells in the logarithmic growth phase, and use fresh RPMI-1640 medium to prepare a density of 2×10 per ml 5 The cell suspension ...

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Abstract

The invention discloses an aromatic geldanamycin derivant, making method, drug composition and application with chemical structure I, wherein R1-R8 is defined as request; the composition can prepare periodical inhibitor and tumour proof agent of cell.

Description

Technical field: [0001] The present invention relates to aromatized geldanamycin derivatives, a method for preparing such compounds by fermentation, a pharmaceutical composition containing such compounds as active ingredients, and the use of such compounds for the preparation of cell cycle inhibitors and cell proliferation inhibitors and the use of antineoplastic drugs. Background technique: [0002] Geldanamycin was first discovered in 1970 from Streptomyces products [C.DeBoer, et al.; Geldanamycin, a new antibiotic: J.Antibiot., 1970, 23(9), 442-447], and later, Many similar compounds have been discovered from microbial products or artificially synthesized and found to have a variety of biological activities. Such as literature [M.Muroi, et al.; The structures of macbecin I and II: Tetrahedron, 1981, 37, pp.1123-1131], literature [R.C.Schnur, et al.; Inhibition of the oncogene product p185 erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D225/06C07D491/04C12P17/10C12P17/18A61K31/395A61K31/357A61P35/00C12R1/465
Inventor 崔承彬韩冰蔡兵
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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