CN106146336A - A kind of compound with anti-breast cancer activity and application thereof - Google Patents
A kind of compound with anti-breast cancer activity and application thereof Download PDFInfo
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- CN106146336A CN106146336A CN201510146090.XA CN201510146090A CN106146336A CN 106146336 A CN106146336 A CN 106146336A CN 201510146090 A CN201510146090 A CN 201510146090A CN 106146336 A CN106146336 A CN 106146336A
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Abstract
The invention discloses a kind of compound with anti-breast cancer activity, its entitled methyl2-(4-fluoro-2-hydroxybenzamido) benzoate, structural formula as I.This compound is that small-molecule chemical thing storehouse is screened in the tumor cell of In vitro culture and obtained, and is evaluated by tumor Model in Nude Mice further.Vivo and vitro test shows, this compound has the strongest inhibitory action to growth and the propagation of breast cancer cell, and can kill tumor cell under low concentration, and to the growth of normal breast cell and no effect on survival.Because of its anticancer effect safe efficient, preferable, the exploitation new types of therapeutic agents for anti-breast cancer can be attempted, have a good application prospect.
Description
Technical field
The present invention relates to compound and application thereof, particularly relate to a kind of compound with anti-breast cancer activity
And application, belong to biomedical sector.
Background technology
Breast carcinoma is the major malignant tumor of harm WomanHealth, is the cancer class that Chinese women sickness rate is the highest
Type, its sickness rate is in gesture in cumulative year after year in recent years, and rejuvenation trend is notable.Expect the year two thousand thirty,
China's women with breast cancer morbidity number will reach 23.4 ten thousand examples, and neopathy rate growth rate is the 2 of world average level
Times, average age of onset 10-15 more Zao than western countries, and 5 years survival rates are only 50%-60%.According to dividing
Sub-hypotype and Immunohistochemical, can be divided into 4 classes clinically by breast carcinoma: Luminal A type
(ER+/PR+, HER-2-), Luminal Type B (ER+/PR+, HER-2+), HER-2+ type (ER-/PR-/
And Basal-like type (ER-/PR-/HER-2-) HER-2+).The clinical treatment of different molecular hypotype breast carcinoma is anti-
Should be different with life cycle, increasingly cause clinical attention.It is currently used for treating breast carcinoma means and mainly has hands
Art treatment, radiotherapy, chemotherapy etc..Wherein operative treatment risk is high, big to human body wound,
Make patient's immunity reduce, disease resistance is declined, is only applicable to early stage patient.Radiotherapy is to tumor
Partial controll effect poor, can kill the normal structure to irradiated region, also may result in weak, nauseating etc. simultaneously
The iatrogenic injury such as systemic adverse reactions or radiation myelitis.Chemotherapy is to treat breast carcinoma the most
Means widely, but there is many thorny problems in traditional anti-breast cancer chemotherapeutics: 1. suppress the life of tumor
Length is notable or cannot significantly kill tumor cell；2. suppressing growth of tumour cell or killing cancerous cell
Meanwhile, the various types of cells of breeding normal in body is also had toxic and side effects in various degree, and easily cause and exempt from
The destruction of epidemic disease system；3. couple some patient with breast cancer produces drug resistance；4. single medicine cannot kill not simultaneously
Breast cancer cell with molecular isoform.Therefore a kind of new chemotherapeutics is found very urgent, will be to breast carcinoma
Treatment there is important practice significance.
Summary of the invention
In view of this, in order to solve the problems referred to above, what present invention screening obtained has the one of anti-breast cancer activity
Planting compound, its entitled methyl 2-(4-fluoro-2-hydroxybenzamido) benzoate, molecular formula is shown in
I.This compound can significantly inhibit growth and the survival of each molecular isoform breast cancer cell, and can effectively suppress little
The propagation of Mus in-vivo tumour, points out it to have important development and application in breast carcinoma clinical treatment and is worth,
Can attempt being prepared as the medicine of anti-breast cancer treatment.
Accompanying drawing explanation
In order to make the object, technical solutions and advantages of the present invention clearer, below in conjunction with accompanying drawing to this
Bright it is described in further detail, wherein:
Fig. 1. this compound is to people normal breast cell strain MCF-10A and each molecular isoform breast carcinoma cell strain
Growth and the detection of survival inhibitory action.
Fig. 2. the detection to mouse interior tumor growth inhibited effect of this compound.
Detailed description of the invention
1) compound suppresses growth and the survival of each molecular isoform breast carcinoma cell strain.
By normal breast cell strain MCF10A and each molecular isoform breast carcinoma cell strain MDA231, MCF7,
T47D and SKBR3 is inoculated in 96 orifice plates with 10,000 cell per well.Second day adds concentration is 1 μM
Compound and the PBS (matched group) of same volume, after 48 hours useAQueousDan Rong
Liquid cell proliferation detecting kit (Promega company) quantitative determines the proliferative conditions of each process group cell；
WithLuminescence method cell viability detection kit (Promega company) quantitative determines each process
The number of group living cells.This both of which is single agents to be directly added in the cultivation cell containing serum,
Without washed cell, remove culture medium or carry out multistep sample-adding operation.A) in cell proliferating determining is tested,
Every hole 100ul culture medium adds 20 μ l37 after AQueous One Solution Reagent
DEG C, hatch in the environment of 5%,CO2 4 hours, then 490nm reads absorbance.B) deposit at cell
Live in determination experiment, on 96 orifice plates, addAfter reagent mixing, logical in 10 minutes
Cross luminometer to detect.
Result shows that the growth of people normal breast cell strain MCF-10A and survival are not affected by this compound,
But it is notable (Fig. 1) to the inhibitory action of the growth of each molecular isoform breast carcinoma cell strain and survival.Wherein Figure 1A
For this compound, people normal breast cell strain MCF-10A and the growth of each molecular isoform breast carcinoma cell strain are pressed down
The detection made；Figure 1B is that this compound is to people normal breast cell strain MCF-10A and each molecular isoform
The detection of breast carcinoma cell strain survival inhibitory action.
2) growth of people source breast cancer cell in compound suppression Mice Body.
Raise 60 6-8 week Reconstruction in Sever Combined Immunodeciency (SCID) female mices, body weight 20 ± 2 grams.By 1
Million MDA231 mankind mastopathy cell right axil subcutaneous vaccination to every mices.After 10 days, long etc. tumor
To general 200mm3, it is randomly divided into 3 groups, often group 20.First group is matched group, every other day abdominal cavity
Inject 100 μ lPBS；Second group every other day lumbar injection 100 μ l concentration be the compound of 5mg/kg body weight；
3rd group every other day lumbar injection 100 μ l concentration be the compound of 10mg/kg body weight.The most continuous
Inject 4 weeks, measured a tumor size every 3 days.After surrounding, tumor-bearing mice is put to death, take subcutaneous tumors
Block, claims tumor weight, calculates tumour inhibiting rate as follows: tumour inhibiting rate (IR)=[matched group tumor weighs in (g)-medication group tumor
(g)]/matched group tumor weight (g) × 100%.Result shows, this compound is in 5mg/kg body weight and 10mg/kg body weight
Under two kinds of dosage, all the growth of mouse tumor can there be obvious inhibitory action, and agent effect relationship substantially (figure
2)。
The foregoing is only the preferred embodiments of the present invention, be not limited to the present invention, it is clear that this area
Technical staff the present invention can be carried out various change and modification without departing from the spirit and scope of the present invention.
So, if these amendments of the present invention and modification belong to the scope of the claims in the present invention and equivalent technologies thereof
Within, then the present invention is also intended to comprise these change and modification.
Claims (3)
1. there is the compound of structure shown in Formulas I:
2. the purposes in preparing anti-breast cancer medicines of the compound shown in claim 1.
3. an anti-breast cancer compound, it is characterised in that: described anti-breast cancer medicines is with claim 1
Described compound is active component, adds the preparation that pharmaceutical carrier is made.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510146090.XA CN106146336A (en) | 2015-03-24 | 2015-03-24 | A kind of compound with anti-breast cancer activity and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510146090.XA CN106146336A (en) | 2015-03-24 | 2015-03-24 | A kind of compound with anti-breast cancer activity and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106146336A true CN106146336A (en) | 2016-11-23 |
Family
ID=57340060
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| Application Number | Title | Priority Date | Filing Date |
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| CN201510146090.XA Pending CN106146336A (en) | 2015-03-24 | 2015-03-24 | A kind of compound with anti-breast cancer activity and application thereof |
Country Status (1)
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1886365A (en) * | 2003-11-25 | 2006-12-27 | 诺沃挪第克公司 | Novel salicylic anilides |
| JP2010053060A (en) * | 2008-08-27 | 2010-03-11 | Kansai Univ | Anticancer agent having acylaminophenyl group |
| WO2014113467A1 (en) * | 2013-01-15 | 2014-07-24 | Board Of Regents, The University Of Texas System | Stat3 inhibitor |
| US20140221411A1 (en) * | 2011-10-21 | 2014-08-07 | Korea Research Institute Of Bioscience And Biotechnology | 2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient |
| CN103980152A (en) * | 2014-05-30 | 2014-08-13 | 西安交通大学 | Benzamide compound with antitumor activity as well as preparation method and application thereof |
-
2015
- 2015-03-24 CN CN201510146090.XA patent/CN106146336A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1886365A (en) * | 2003-11-25 | 2006-12-27 | 诺沃挪第克公司 | Novel salicylic anilides |
| JP2010053060A (en) * | 2008-08-27 | 2010-03-11 | Kansai Univ | Anticancer agent having acylaminophenyl group |
| US20140221411A1 (en) * | 2011-10-21 | 2014-08-07 | Korea Research Institute Of Bioscience And Biotechnology | 2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient |
| WO2014113467A1 (en) * | 2013-01-15 | 2014-07-24 | Board Of Regents, The University Of Texas System | Stat3 inhibitor |
| CN103980152A (en) * | 2014-05-30 | 2014-08-13 | 西安交通大学 | Benzamide compound with antitumor activity as well as preparation method and application thereof |
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Application publication date: 20161123 |