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USE OF 3-O-SULFAMOYLOXY-7[beta]-METHYL-D-HOMO-6-OXAESTRA-1,3,5(10),8(9)-TETRAEN-17A-ONE TO TREAT BREAST CANCER

A sulfamoyloxy, breast cancer technology, applied in the field of medicine

Pending Publication Date: 2022-02-01
纳塔利娅爱德华多夫娜伊利娅索娃
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, estrone sulfamate inhibits estrone sulfatase, but release of the free hormone leads to the emergence of strong uterotropic activity [Shields-Botella J. et al., J. Steroid Biochem. Mol. Biol., 2003 , Vol. 84, pp. 327-335]

Method used

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  • USE OF 3-O-SULFAMOYLOXY-7[beta]-METHYL-D-HOMO-6-OXAESTRA-1,3,5(10),8(9)-TETRAEN-17A-ONE TO TREAT BREAST CANCER
  • USE OF 3-O-SULFAMOYLOXY-7[beta]-METHYL-D-HOMO-6-OXAESTRA-1,3,5(10),8(9)-TETRAEN-17A-ONE TO TREAT BREAST CANCER
  • USE OF 3-O-SULFAMOYLOXY-7[beta]-METHYL-D-HOMO-6-OXAESTRA-1,3,5(10),8(9)-TETRAEN-17A-ONE TO TREAT BREAST CANCER

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0036] Synthesis of 3-hydroxy-7β-methyl-D--6-oxygen-1,3,5 (10), 8 (9), 8, 14-pentane-17a-ketone (5).

[0037]The open loop compound of formula 4 was prepared from 6.0 g of a full ketone (3).

[0038] The open-loop steroids in formula 4 were added 6 ml of hydrochloric acid in 100 ml of methanol, and the resulting mixture was boiled for 10 hours. The cooled reaction mixture was poured into cold water, washed with 5% sodium hydrogencarbonate, and then washed to neutral pH, and dried over sodium sulfate. The solvent is distilled on a rotary evaporator. The melting point of the resulting product was 237-240 ° C.

[0039] NMR spectrum 1 Н (CDCL 3 ), ppm: 7.08; 6.45; 6.39; 5.84; 5.30; 5.00, adoption (1н, C3-OH); 2.79; 2.74-2.40; 2.4, 1.69; 1.28; 1.24, (3H).

[0040] NMR spectrum 13 С (DMSO-D 6 PPM: 214.6; 158.6, 152.6 (с -3, с-5), 137.4; C); 123.9, 125.4; 124.1; 115.7; 118.3; 108.7; 103.8; 69.9; 45.0; 35.4; 28.6; 24.1; 21.1; 18.1.

[0041] 3-hydroxy-7β-methyl-D-Tie-6-oxy-7β-methyl-D-Die-...

example 2

[0048] Study on pharmacological activity.

[0049] Cell culture and culture conditions.

[0050] The cultured cultured cultured MCF-7 human cell culture was studied. Normal human skin fibroblasts (HDF) was used as a negative control using the normal human skin of early pass.

[0051] The 1.0% non-antibiotic fetal bull embryo (Biolot) added in a 5% carbon dioxide atmosphere was used in a 5% carbon dioxide atmosphere, and the cells were carried out in the DMEM / F12 medium (Biolot). nourish.

[0052] Evaluation of proliferative activity of cells.

[0053] 50x10 per bottle 4 Cells in the Carrell bottle. In order to study the proliferation activity under sulfate enzyme inhibitory conditions, 24 hours after inoculation, the medium is replaced with a medium containing a sulfate enzyme inhibitor, and the final concentration is 50 ml / ml, and then these tumor cell lines are incubated. The time period (24 to 72 hours). The inhibitor is dissolved in dimethyl sulfoxide (DMSO). The final con...

example 3

[0059] This study was carried out against the conventional category of HER-2 / NEU generated female FVB mice obtained from Charles River Laboratories (Italy) mouse library. At the beginning of the study, animals were 21-41 weeks, with weight of 25-30 grams.

[0060] Tamoxifen Hexal (Germany Holz, Germany) was used in the experiment. A circular double convex tablet has a uniform smooth surface comprising 20 mg of active compounds.

[0061] Residential conditions are based on the standards specified in Ilar Publication, 1996, Nationalacademy Press, 1996.

[0062] Animals were in groups in a separate T2 cage suitable for laboratory rodents (no more than 5 animals per group) in a separate room. The size of the cage is 268 × 215 × 141 cubic millimeters (the bottom area is 370 square centimeter), which is equipped with a polycarbonate bucket, a stainless steel cover and a drinking water bottle separator with feed containers.

[0063] The cage is made of dust-free shavings.

[0064] Thes...

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Abstract

The invention relates to the field of medicine and to the chemical and pharmaceutical industry, and concerns agents for treating breast cancer. Described is the use of 3-O-sulfamoyloxy-7[beta]-methyl-D-homo-6-oxaestra-1,3,5(10),8(9)-tetraen-17a-one as an anti-cancer agent in monotherapy and adjuvant therapy for breast cancer, including triple-negative breast cancer.

Description

Technical field [0001] The present invention relates to the field of medicine and chemistry and pharmaceutical industries, and involves a drug for treating breast cancer. Background technique [0002] Breast cancer is a major tumor disease in women [Parkin D.M., Bray F., Ferlay J., Pisanip., Ca Cancer J. Clin, 2005, Vol. 55, Page 74-108]. According to the data of WHO, 2090,000 patients around the world, the annual death of the death is 627,000 women [http: / / www.who.int / news-room / FACT-SHETS / detail / cancer] . [0003] A large part of the tumor in this position is developed under the action of estrogen [Yue W., YAger JD, WANG J.-P., Jupe Er, Santen RJ, Steroids, 2013, Volume 78 Page 161-170]. The immunohistochemical analysis revealed breast cancer expressions expressing estrogen (ER), progesterone (PR) and Her2Neu (enabling cancer "Hopsin sensitivity"). A large part of the tumor has ER, PR, and / or HER2NEU 3+. If a tumor is not Er and PR and is not sensitive to Hecein (ER0, PR0, HER...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/566A61P35/00C07J73/00
CPCA61P35/00A61K31/352A61K31/138C07J73/003A61K2300/00A61K31/566C07D311/78
Inventor 沙米尔·肖诺维奇·伊利亚索夫亚历山大·格里戈里耶维奇·沙夫瓦斯韦特兰娜·尼古拉耶芙娜·莫罗兹基娜
Owner 纳塔利娅爱德华多夫娜伊利娅索娃