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Carbonyl additive derivative of geldanamycin benzoquinone, preparation method and use thereof

A geldanamycin and benzoquinone carbonyl technology, which is applied to the carbonyl addition derivatives of geldanamycin-like benzoquinones and their preparation and use, and can solve the problems of derivatives that have not yet been seen

Inactive Publication Date: 2007-03-14
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, among all the geldanamycin compounds that have been recorded in the literature so far, no derivatives formed by the addition of the benzoquinone carbonyl of this type of compound have been seen.

Method used

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  • Carbonyl additive derivative of geldanamycin benzoquinone, preparation method and use thereof
  • Carbonyl additive derivative of geldanamycin benzoquinone, preparation method and use thereof
  • Carbonyl additive derivative of geldanamycin benzoquinone, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Fermentative production and separation and purification of embodiment 1 compound 1

[0079] Fermentation production

[0080] Toxin-producing bacteria The toxin-producing bacteria used to ferment and produce Compound 1 in this example was isolated from soil samples collected from Xishuangbanna and identified as Streptomyces pseudoverticillus (Streptomyces pseudoverticillus) strain YN17707 CGMCC No.1452 through taxonomic studies.

[0081]Fermentative culture of toxin-producing bacteria According to the conventional method of cultivating microorganisms, an appropriate amount of Streptomyces pseudoverticillus (Streptomyces pseudoverticillus) YN17707 CGMCC No.1452 strain was taken, and inoculated into an eggplant-shaped bottle on the Gaoshi Synthetic No. 1 agar solid slant medium, at 28 Activation and culture for 7 days in a Celsius incubator. Get the eggplant-shaped bottle slope that has been activated and cultivated for 7 days, add 15 milliliters of sterile water, scrape ...

Embodiment 2

[0091] Example 2 Cell Cycle Inhibitory Activity Test of Compound 1

[0092] Experimental samples and experimental methods

[0093] Preparation of the test sample solution The test sample is the pure compound 1 isolated and refined in the above-mentioned Example 1. Accurately weigh an appropriate amount of sample, and use methanol to make a solution of the required concentration for testing the activity.

[0094] The subculture activity test of cell lines and cells adopts the temperature-sensitive mouse breast cancer tsFT210 cell line, and the cells are relayed in RPMI-1640 medium containing 10% FBS in a cell incubator with 5% carbon dioxide at 32 degrees Celsius subculture.

[0095] Flow Cytometry Activity Assay Method

[0096] asynchronous culture test

[0097] 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 of each cell was inoculated in a 24-well cell culture plate at 0.5 m...

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Abstract

The present invention relates to geldanamycin type carbonyl radical added benzoquinone derivative and its preparation process as well as the medicine composition with the compound as active component and its use. The compound is prepared through fermentation with, say, pseudostreptoverticillium, and it is proved experimentally that the compound may be used in preparing cell period inhibitor and antitumor preparation.

Description

Technical field: [0001] The present invention relates to a carbonyl addition derivative of geldanamycin-like benzoquinone, a method for preparing the compound by fermentation, a pharmaceutical composition containing the compound and the use of the compound in the preparation of cell cycle inhibitors, cell proliferation inhibitors agents and 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: J.Med.Ch...

Claims

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Application Information

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IPC IPC(8): C07D225/06A61K31/395C12N1/20C12P17/10A61P35/00
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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