CN109432095A - A kind of medical usage of thiazoline derivative - Google Patents
A kind of medical usage of thiazoline derivative Download PDFInfo
- Publication number
- CN109432095A CN109432095A CN201811606086.7A CN201811606086A CN109432095A CN 109432095 A CN109432095 A CN 109432095A CN 201811606086 A CN201811606086 A CN 201811606086A CN 109432095 A CN109432095 A CN 109432095A
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- CN
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- Prior art keywords
- thiazoline derivative
- thiazoline
- derivative
- squamous cell
- cell carcinoma
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a kind of medical usages of thiazoline derivative.Modern science is gradually disclosing the generation essence of malignant tumour, and anti-tumor drug research has entered a new stage.The research success of the drugs such as taxol, shows to continually look for novel mechanism and the cytotoxic drug of unique chemical moieties is still significant.Thiazoline derivative provided by the invention is to the tumour cell except human mouth squamous cell carcinoma Tca8113 without obvious inhibiting effect；Most of thiazoline derivative can significantly inhibit the proliferation of human mouth squamous cell carcinoma Tca8113.Present invention explanation, the parent nucleus and substituent group of thiazoline derivative all significantly affect its inhibiting effect to tumour cell.
Description
Technical field
The invention belongs to field of medicaments, and in particular to a kind of medical usage of thiazoline derivative.
Background technique
The mankind there has been huge progress by unremitting effort in decades, the drug therapy of malignant tumour.Modern section
Learn, the especially fast development of life science, gradually disclose malignant tumour generation essence, anti-tumor drug research into
Enter a new stage.The research success of the drugs such as taxol, shows to have continually looked for novel mechanism and unique chemical moieties
Cytotoxic drug it is still significant.New type antineoplastic medicine for example growth factor receptor inhibitors, angiogenesis inhibitor,
Before biological response modifiers, tumor drug resistance reversal agent, telomerase inhibitor, genetically engineered drug etc. have good research and development
Scape controls the treatment of malignant tumour from table and moves towards radical cure.
But since the pathogenesis of malignant tumour is extremely complex, to reach really to cure also needs a very long mistake
Journey, this needs to continually develop new anticancer drug in the process.
Summary of the invention
The purpose of the present invention is to provide a kind of medical usages of thiazoline derivative.
Realize that above-mentioned purpose technical solution of the present invention is as follows:
The thiazoline derivative of following chemical structure is used to prepare the purposes of the drug for the treatment of human mouth squamous cell carcinoma.
Wherein, R=Me or Bn.
A kind of pharmaceutical preparation for treating human mouth squamous cell carcinoma, with acceptable auxiliary material on active constituent and pharmacy
Acceptable dosage form in pharmacy is made, the active constituent is above-mentioned thiazoline derivative.
Further, the auxiliary material is solid, semisolid or Auxiliary Liquid Material.
Further, the dosage form preferred tablet, capsule, injection.
The thiazoline derivative of following chemical structure is used to prepare the purposes of the drug for the treatment of human mouth squamous cell carcinoma.
Wherein, R=Me, Ph or Bn.
A kind of pharmaceutical preparation for treating human mouth squamous cell carcinoma, with acceptable auxiliary material on active constituent and pharmacy
Acceptable dosage form in pharmacy is made, the active constituent is above-mentioned thiazoline derivative.
Further, the auxiliary material is solid, semisolid or Auxiliary Liquid Material.
Further, the dosage form preferred tablet, capsule, injection.
Outstanding advantages of the invention:
Thiazoline derivative provided by the invention is to the tumour cell except human mouth squamous cell carcinoma Tca8113 without bright
Aobvious inhibiting effect；Most of thiazoline derivative can significantly inhibit the proliferation of human mouth squamous cell carcinoma Tca8113.Thiazole
The parent nucleus and substituent group of quinoline derivant all significantly affect its inhibiting effect to tumour cell.
Detailed description of the invention
Fig. 1 is IC50 value of each thiazoline derivative to human mouth squamous cell carcinoma Tca8113 Proliferation Ability.
Specific embodiment
Just specifically introduce essentiality content of the invention in conjunction with the embodiments below, due to length, experimentation is retouched
Stating can not accomplish very in detail, and the part being not described in detail in all experiments is conventional behaviour well known to those skilled in the art
Make.
One, experimental material
Human lung adenocarcinoma cell H2228, human bladder cancer cell T24, human liver cancer cells Hep G2, human breast cancer cell
MCF-7, gastric carcinoma cells MGC-803, human mouth squamous cell carcinoma Tca8113 are respectively with the RPMI- containing 10% fetal calf serum
1640 cultures are based on 37 DEG C, 5%CO2Logarithmic growth phase cell is selected in routine culture in cell incubator, experiment.
Thiazoline derivative self-control or purchase, purity > 98%, chemical structure is as shown in the table.
RPMI-1640 culture medium, fetal calf serum are purchased from Gibco.
Two, experimental method
Each thiazoline derivative is tested to the inhibited proliferation of each cancer cell, according to thiazoline derivative using mtt assay
Its anticancer effect, specific steps are evaluated to the IC50 value of each cancer cell multiplication inhibitory activity are as follows: by each cancer cell inoculation to containing
In 96 orifice plates of RPMI-1640+10% fetal calf serum culture medium, 37 DEG C, 5%CO2CMC model for 24 hours, is added into culture plate
The thiazoline derivative of the diluted gradient concentration of culture medium and blank control handle 72h, then it is 5mg/mL that concentration, which is added, to every hole
20 μ L of MTT reagent, continue cultivate 4h, abandon supernatant, then to every hole be added 150 μ L DMSO, oscillation dissolution, using microplate reader
The absorbance value (OD570) under 570nm wavelength is measured, calculates each thiazoline derivative according to the following formula to each inhibition of cancer cell
Rate, Graphpad fitting acquire IC50 value.
Inhibiting rate (%)=(blank control group OD570- experimental group OD570)/blank control group OD570 × 100%
Three, experimental result
The IC50 value that each thiazoline derivative inhibits each cancer cell multiplication is as shown in table 1 and Fig. 1.
The IC50 value that each thiazoline derivative of table 1 inhibits each cancer cell multiplication
It is above-mentioned the experimental results showed that, each thiazoline derivative is thin to the tumour except human mouth squamous cell carcinoma Tca8113
Born of the same parents are without obvious inhibiting effect；In thiazoline derivative, except thiazoline derivative 2 can significantly inhibit human mouth squamous cell
The proliferation of cancer Tca8113.The parent nucleus and substituent group of thiazoline derivative all significantly affect its inhibiting effect to tumour cell.
Above-described embodiment is the embodiment to essentiality content of the present invention, for preferably explaining the present invention, but this field skill
Protection scope of the present invention it is to be understood that above-mentioned specific embodiment should not be confined to by art personnel.
Claims (4)
1. the purposes that the thiazoline derivative of following chemical structure is used to prepare the drug for the treatment of human mouth squamous cell carcinoma.
Wherein, R=Me or Bn.
2. a kind of pharmaceutical preparation for treating human mouth squamous cell carcinoma, with acceptable auxiliary material system on active constituent and pharmacy
At acceptable dosage form in pharmacy, it is characterised in that: the active constituent is derivative for thiazoline described in claim 1
Object.
3. pharmaceutical preparation according to claim 2, it is characterised in that: the auxiliary material is solid, semisolid or Auxiliary Liquid Material.
4. pharmaceutical preparation according to claim 2, it is characterised in that: the dosage form preferred tablet, capsule, injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811606086.7A CN109432095B (en) | 2018-12-27 | 2018-12-27 | Medical application of thiazoline derivative |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811606086.7A CN109432095B (en) | 2018-12-27 | 2018-12-27 | Medical application of thiazoline derivative |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109432095A true CN109432095A (en) | 2019-03-08 |
| CN109432095B CN109432095B (en) | 2021-01-15 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811606086.7A Active CN109432095B (en) | 2018-12-27 | 2018-12-27 | Medical application of thiazoline derivative |
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| Country | Link |
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| CN (1) | CN109432095B (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103864785A (en) * | 2014-03-11 | 2014-06-18 | 中国农业大学 | Thiazoline derivatives with aza-indole framework as well as preparation method and application thereof |
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2018
- 2018-12-27 CN CN201811606086.7A patent/CN109432095B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103864785A (en) * | 2014-03-11 | 2014-06-18 | 中国农业大学 | Thiazoline derivatives with aza-indole framework as well as preparation method and application thereof |
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| CN109432095B (en) | 2021-01-15 |
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| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: Cang Huaiqin Inventor after: Liu Huaping Inventor after: Li Yuequn Inventor after: Jin Rong Inventor before: Liu Huaping Inventor before: Li Yuequn Inventor before: Jin Rong |
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Effective date of registration: 20201229 Address after: 266555 No. five mountain road, Huangdao District, Qingdao, Shandong, 1677 Applicant after: THE AFFILIATED HOSPITAL OF QINGDAO University Address before: 211198 18 Jiangning Science Park, Nanjing, Jiangsu. Applicant before: NANJING GAISIFU MEDICAL TECHNOLOGY Co.,Ltd. |
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