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49 results about "Brefeldin A" patented technology
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Brefeldin A is a lactone antiviral produced by the fungus Penicillium brefeldianum. Brefeldin A inhibits protein transport from the Golgi apparatus to the endoplasmic reticulum indirectly by preventing association of COP-I coat to the Golgi membrane. Brefeldin A was initially isolated with hopes to become an antiviral drug but is now primarily used in research to study protein transport.
Brefeldin A ester derivatives and their preparation method and use
ActiveCN103788053ASimple methodHigh inhibition rateOrganic active ingredientsOrganic chemistryKidney cancerEsophagus Cancers
The invention provides brefeldin A ester derivatives having antitumor activity and their preparation method and use. The brefeldin A ester derivatives have structures shown in the structural general formula (I). The brefeldin A ester derivatives have high effects on esophagus cancer, lung cancer, kidney cancer, colorectal cancer and prostatic cancer and have an in-vitro detection effective inhibition rate of 80%. The preparation method of the brefeldin A ester derivatives has simple processes and can be operated easily.
Owner:ZHEJIANG UNIV OF TECH
Eupenicillium brefeldianum variety ZJB082702 and application thereof in preparation of Brefeldin A by fermentation
The invention provides a Brefeldin A high-yield strain-Eupenicillium brefeldianum variety ZJB082702 and an application thereof in preparation of Brefeldin A by fermentation. The Eupenicillium brefeldianum variety ZJB082702 is collected in China Center for Typical Culture Collection, the address of the center: Wuhan University, Wuhan, China, 430072, the accession data is July 31, 2008, and the accession number is CCTCC No: M 208113. The use of the strain for preparing the Brefeldin A by fermentation has higher yield, and the maximum concentration of the Brefeldin A can achieve 943.8mg / L of fermentation broth.
Owner:ZHEJIANG UNIV OF TECH
Brefeldin A ester derivatives, and preparation and application thereof
ActiveCN105153136AHas antioxidant activityHas antitumor activityOrganic chemistryAntinoxious agentsDiseaseDrug development
The invention discloses brefeldin A ester derivatives, and preparation and application thereof. The brefeldin A ester derivative compounds have antioxidation activity and antitumor activity, wherein the brefeldin A ester derivative compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable antioxidation effect and can remove DPPH, ABTS and super oxygen free radical (O2<->), and the compound (I-7) has better removal effect on DPPH, ABTS and super oxygen free radical (O2<->) than vitamin E; and the compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable inhibition activity for human lung cancer cells A549. Therefore, the result shows that the derivatives have wide application prospects in the drug development system, provide a new and broader idea for synthesizing and screening BFA (brefeldin A) derivative drugs and provide a more efficient way for treating related diseases.
Owner:ZHEJIANG UNIV OF TECH
Brefeldin A derivatives, and preparation method and uses thereof
The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by modification on 7-site of brefeldin A. Particularly, the invention relates to 7-site furazan NO donor substituted brefeldin A derivatives, and a preparation method of the derivatives and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.
Owner:SHENYANG PHARMA UNIVERSITY
Plant endophytic fungus Eupenicillium brefeldianum F4a and its application
ActiveCN104877910AImprove antibacterial propertiesImprove insecticidal abilityOrganic active ingredientsBiocideBiotechnologyEupenicillium
The invention relates to the technical field of microbes, and concretely relates to a new plant endophytic fungus and its application in the preparation of brefeldin A (BFA). The plant endophytic fungus is Eupenicillium brefeldianum F4a, and is preserved in China Center for Type Culture Collection on Dec. 18, 2012 with the preservation number of CCTCC M2012531. The Eupenicillium brefeldianum F4a can generate high content BFA, and the highest fermentation output reaches 1.9g / L. The invention also provides a method for preparing the highly pure BFA through HP20 solid phase extraction and rapid silica gel column chromatography or a pure crystallization technology. The method has the advantages of low production cost, great reduction of treatment and pollution of organic matters, and good industrial prospect. The BFA prepared in the invention has antifungal and insecticidal activity, and is an ideal veterinary or agricultural candidate drug.
Owner:SHENYANG INST OF APPLIED ECOLOGY - CHINESE ACAD OF SCI
Brefeldin A-producing bacteria and method for preparing brefeldin A by fermentation
The invention relates to Brefeldin A-producing bacteria, a preparation method, a method for preparing the brefeldin A by fermentation and the application thereof. The Brefeldin A-producing bacteria has the advantages of easy selection, cultivation and storage, low cost, simple process, short preparation period, high yield, no usage of toxic raw material, less organic solvent, thorough guarantee of medicine resource, potential of mass production and favorable economic and social benefits, contributes to the maintenance of ecological balance and the protection of natural resources. The fermentation product of the invention, of which the main component is THSG, develops novel medical application, the Brefeldin A has high safety, low toxicity, stable property, stronger pharmacological action, simple preparation process, high yield and considerably wide range of application, is multipurpose, and can provide a novel source for medicines for preventing, diagnosing, detecting, protecting, curing and researching antimycotic, antiviral and antineoplastic diseases and the directly related diseases.
Owner:SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
4,7-site difurazan NO donor substituted derivatives of brefeldin A, and preparation method and uses thereof
The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by simultaneous modification on 4-site and 7-site of brefeldin A. Particularly, the invention relates to 4,7-site difurazan NO donor substituted brefeldin A derivatives, and a preparation method of the derivatives and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.
Owner:SHENYANG PHARMA UNIVERSITY
Methods of Treating Serosal Cancer
InactiveUS20150030583A1Improve the quality of lifeProlong survival timeHalogenated hydrocarbon active ingredientsBiocidePanobinostatNVP-AUY922
The discovery of clonally pure populations of serosal cancer stem cells (CSCs) as well as methods of producing CSCs, culturing the CSCs and using them in screening assays, has lead to the development of methods of treating serosal and ovarian cancers by targeting removal or inhibition of the glycocalyx coat surrounding such cells, and includes combination therapies using particular chemotherapeutics in conjunction with glycocalyx inhibitors, as well as the same new chemotherapy treatments without targeting the glycocalyx, where the chemotherapeutic agent is any one of LBH-589 (Panobinostat), NVP-AUY922, LAQ824 (NVP-LAQ824, Dacinostat), colchicine, brefeldin A, diphenyleneiodonium chloride, any combination thereof or another agent identified herein. These treatment methods of the invention can also be used in combination with radiation treatment or other conventional cancer therapy.
Owner:SLOAN KETTERING INST FOR CANCER RES
Compounds used for treating cancer and the use thereof
The present invention discloses compounds for the treatment of cancer and its application. These compounds comprises one of the following compound: Ammonium pyrrolidinedithiocarbamate Bay 11-7085 BIO Brefeldin A (+)-Butaclamol Calcimycin Calmidazoliur chloride Chelerythrine chloride CK2 Inhibitor 2 CGP-74514A hydrochloride CGS-12066A meleate Dequalinium dichloride Dihydroouabain Diphenyleneiodonium chloride Emetine dihydrochloride hydrate GR 127935 hydrochloride Nifedipine 6-Nitroso-1,2-benzopyrone Palmitoyl-DL-Carnitine chloride Parthenolide PD 169316 1,10-Phenanthroline monohydrate 4-Phenyl-3-furoxancarbonitrile Prazosin hydrochloride Protoporphyrin IX disodium Quinacrine dihydrochloride Quabain Retinoic acid p-hydroxyanilide Rottlerin Sanguinarine chloride Tetraethylthium disulfide and SU 9516. The invention also provides new uses of these compounds, compounds such as for the preparation of the treatment of cancer, inhibit cancer cell, cancer stem cell growth and provides a new pharmaceutical composition for treating cancers
Owner:NAT DEFENSE MEDICAL CENT
Brefeldin A glycosylated derivative and preparation and application thereof
InactiveCN103739644AGood water solubilityRetains tumor suppressor activityOrganic active ingredientsSugar derivativesSolubilityCancer cell
The invention discloses a brefeldin A glycosylated derivative shown in a formula (I) and a preparation method and application thereof. The invention provides a novel brefeldin A glycosylated derivative; the water solubility of the brefeldin A glycosylated derivative is enhanced; the tumor inhibiting activity of the brefeldin A is retained; in-vitro detection shows that the effective inhibition rate to cancer cells such as a human esophagus cancer and the like can be up to 80%; the preparation method of the preferred brefeldin A glycosylated derivative is obtained by optimizing the conditions of a compound (II), (img file='DDA0000451154560000011.TIF' wi='776' he='307' / ), in the formula (I), R is pentose, hexose, amino hexose or hexose acid.
Owner:ZHEJIANG UNIV OF TECH
Brefeldin A and derivative and application thereof
ActiveCN105566277AStrong anti-HIV latent activityEasy to removeOrganic active ingredientsOrganic chemistryInfected cellFermentation
The invention discloses brefeldin A (BFA) and a derivative and application thereof. The brefeldin A has the extremely high anti-HIV latency activity, and the series compound is obtained through a static culture fermentation method and chemical modification. The brefeldin A and the derivative thereof are of a structure shown as a formula (I) (please see the formula in the description), wherein R1-R5 represent H, OH, CH3, OCH3 and (OCH3)2 or OCOCH3 respectively, and R6 represents CH3. The brefeldin A and the derivative thereof can serve as anti-HIV latency drugs and can be applied to preparation of a drug for treating an AIDS jointly with an antiretroviral drug, when the brefeldin A and the derivative thereof are jointly applied with the antiretroviral drug, the brefeldin A and the derivative thereof can enable latent HIVs in infected cells to be expressed, have the effect of intervening HIV latency and can clear the activated and infection-latent cells to accelerate clearance of a latent virus storage, and the wide application prospect is achieved.
Owner:浙江美新控股有限公司
Penicillium ochrochloron and its application in preparation of brefeldin A
InactiveCN104711198AValuable strain resourcesFungiMicroorganism based processesMicroorganismPharmacy
The invention belongs to the technical filed of microbes, and concretely relates to Penicillium ochrochloron and its application in the preparation of brefeldin A. A technical problem to be solved in the invention is providing a new choice for production of BFA through biological fermentation. A bacterial strain produced in the invention is Penicillium ochrochloron SWUKD4.211, and has a preservation number of CCTCC M2015022. The invention also provides a method for producing the BFA by adopting Penicillium ochrochloron fermentation. The BFA production ability of the bacterial strain obtained through the method can reach 356.0mg / L, and the method provides a new choice for the production of the BFA, provides a precisou strain for biological pharmacy, and has great application values.
Owner:SOUTHWEST UNIVERSITY
7-amide-brefeldin a derivative as well as preparation method and application of 7-amide-brefeldin a derivative
InactiveCN104529991AHigh inhibition rateSimple methodOrganic active ingredientsTripeptide ingredientsKidney cancerMedicine
The invention relates to a 7-amide-brefeldin A derivative with anti-tumor activity as well as a preparation method and application of the 7-amide-brefeldin A derivative. The 7-amide-brefeldin A derivative serving as a novel compound provided by the invention has a high effect on treating liver cancer, lung cancer, breast cancer, kidney cancer, colorectal cancer and prostate cancer, and has the effective inhibition ratio of 80% through in-vitro detection; and the method for obtaining 7-NH2-brefeldin A and 7-amide-brefeldin A derivatives is simple and easy to operate.
Owner:ZHEJIANG UNIV OF TECH
Polyethylene glycol-brefeldin A ester derivatives and preparation and applications of the derivatives
ActiveCN104788668ASimple methodEasy to operateSynthetic polymeric active ingredientsAntineoplastic agentsKidney cancerMedicine
Polyethylene glycol-brefeldin A ester derivatives are provided. Structures of the derivatives are shown as a formula I, a formula II, a formula III or a formula IV. Applications of the novel compounds in preparation of medicines for treating and preventing liver cancer, lung cancer, breast cancer, kidney cancer, cancer of colon and prostatic cancer are also provided.
Owner:ZHEJIANG UNIV OF TECH
Preparation method and uses of a class of brefeldin A derivative containing chlormethine linked at site 4
ActiveCN110028477AImprove pharmacological activityOrganic active ingredientsOrganic chemistryNitrogen mustardMedicinal chemistry
The invention belongs to the field of natural medicine and medicinal chemistry, and relates to a preparation method and uses of a class of brefeldin A derivative containing chlormethine linked at site4 and having antitumor activity, wherein the brefeldin A derivative containing chlormethine linked at site 4, and the pharmaceutically acceptable salt have a structure represented by the following general formula I, and n is defined in the claim and specification.
Owner:SHENYANG PHARMA UNIVERSITY
Brefeldin A combined anti-cancer compound medicine
InactiveCN105456255AEnhanced inhibitory effectGood effectOrganic active ingredientsAntineoplastic agentsTreatment effectSide effect
The invention discloses a brefeldin A combined anti-cancer compound medicine, aims to provide a brefeldin A combined anti-cancer compound medicine which has low using concentration and small toxic and side effects and has an excellent treatment effect on tumors, in particular prostatic cancer, and belongs to the technical field of medicines. According to the technical key points, the medicine is prepared from brefeldin A combined with taxane drugs.
Owner:GUANGDONG UNIV OF TECH
Preparation and anti-tumor application of 7-N3-brefeldin A and 1,2,3-triazole derivative thereof
ActiveCN104592208AHigh inhibition rateSimple methodOrganic active ingredientsTripeptide ingredientsLung cancerBrefeldin A
The invention relates to preparation and application of 7-N3-brefeldin A with anti-tumor activity and a 1,2,3-triazole compound of the 7-N3-brefeldin A. The compound provided by the invention has an efficient curative effect on liver cancer, lung cancer, breast cancer, renal cancer, colon cancer and prostatic cancer; the effective inhibition rate can be 80% through detection in vitro; and the method for obtaining the 7-N3-brefeldin A and the 1,2,3-triazole compound of the 7-N3-brefeldin A is simple and easy to operate. The chemical formula is as shown in the specification.
Owner:ZHEJIANG UNIV OF TECH
A kind of plant endophytic fungus Penicillium breenensis f4a and its application
ActiveCN104877910BImprove antibacterial propertiesImprove insecticidal abilityBiocideOrganic active ingredientsBacillus thuringiensisEupenicillium
The invention relates to the technical field of microbes, and concretely relates to a new plant endophytic fungus and its application in the preparation of brefeldin A (BFA). The plant endophytic fungus is Eupenicillium brefeldianum F4a, and is preserved in China Center for Type Culture Collection on Dec. 18, 2012 with the preservation number of CCTCC M2012531. The Eupenicillium brefeldianum F4a can generate high content BFA, and the highest fermentation output reaches 1.9g / L. The invention also provides a method for preparing the highly pure BFA through HP20 solid phase extraction and rapid silica gel column chromatography or a pure crystallization technology. The method has the advantages of low production cost, great reduction of treatment and pollution of organic matters, and good industrial prospect. The BFA prepared in the invention has antifungal and insecticidal activity, and is an ideal veterinary or agricultural candidate drug.
Owner:SHENYANG INST OF APPL ECOLOGY CHINESE ACAD OF SCI
Brefeldin A derivative with melphalan-based chlormethine linked at site 4, preparation method and uses thereof
ActiveCN110028482AImprove pharmacological activityOrganic active ingredientsOrganic chemistryAlkylating antineoplastic agentPharmaceutical drug
The invention belongs to the field of natural medicine and medicinal chemistry, and relates to a preparation method and uses of a brefeldin A derivative with melphalan-based chlormethine linked at site 4, specifically to a preparation method for introducing a DNA alkylating agent melphalan derivative at the 4-OH site of brefeldin A, and applications in preparation of antitumor drugs. According tothe present invention, the brefeldin A derivative with melphalan-based chlormethine linked at site 4, and the pharmaceutically acceptable salt have a structure represented by a general formula I, wherein n is defined in the claim and specification.
Owner:SHENYANG PHARMA UNIVERSITY
Eupenicillium brefeldianum variety ZJB082702 and application thereof in preparation of Brefeldin A by fermentation
The invention provides a Brefeldin A high-yield strain-Eupenicillium brefeldianum variety ZJB082702 and an application thereof in preparation of Brefeldin A by fermentation. The Eupenicillium brefeldianum variety ZJB082702 is collected in China Center for Typical Culture Collection, the address of the center: Wuhan University, Wuhan, China, 430072, the accession data is July 31, 2008, and the accession number is CCTCC No: M 208113. The use of the strain for preparing the Brefeldin A by fermentation has higher yield, and the maximum concentration of the Brefeldin A can achieve 943.8mg / L of fermentation broth.
Owner:ZHEJIANG UNIV OF TECH
Preparation method and uses of a class of brefeldin A derivative containing chlormethine linked at site 4 and site 7
ActiveCN110028478AImprove pharmacological activityOrganic active ingredientsOrganic chemistryAntitumor activityNatural medicine
The invention belongs to the field of natural medicine and medicinal chemistry, and relates to a preparation method and uses of a class of brefeldin A derivative containing chlormethine linked at site4 and site 7 and having antitumor activity, wherein the brefeldin A derivative containing chlormethine linked at site 4 and site 7, and the pharmaceutically acceptable salt have a structure represented by the following general formula I, and n is defined in the claim and specification.
Owner:SHENYANG PHARMA UNIVERSITY
Drugs to improve synaptic transmission
InactiveUS7081474B2Improve efficiencyImprove cognitive functionBiocideNervous disorderSynapseMedicine
Peripherally administered Brefeldin A and its analogs and derivatives are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal issues.
Owner:RGT UNIV OF CALIFORNIA
Method for non-therapeutic purpose restoration of immune function of infiltrating T lymphocytes
InactiveCN109294987AFunction increaseBlood/immune system cellsCell culture active agentsT lymphocyteBlocking antibody
Belonging to the technical field of T lymphocyte receptors, the invention provides a method for non-therapeutic purpose restoration of the immune function of infiltrating T lymphocytes. The method includes: mixing an immune function impaired infiltrating T lymphocyte solution with a blocking agent to obtain a blocking agent-containing solution, wherein the blocking agent includes an anti-Tim-3 blocking antibody and / or an anti-PD-1 blocking antibody; mixing the blocking agent-containing solution with an anti-CD3 antibody and an anti-CD28 antibody, and then performing cultivation to obtain a culture; and mixing the culture with Brefeldin A, and performing incubation to obtain immune function restored infiltrating T lymphocytes. The method provided by the invention can restore the immune function of immune function impaired infiltrating T lymphocytes.
Owner:THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
Hydroxyl phosphate amino acid ester derivatives of Brefeldin A, preparation method thereof, and application thereof
InactiveCN102731573BHighly biologically activeImprove biological activityOrganic active ingredientsGroup 5/15 element organic compoundsBioavailabilityPerylene derivatives
Owner:TIANJIN LINMEI TECH
Application of a kind of brefeldin a in the preparation of inflammatory factor activity inhibitor medicine
ActiveCN110151755BReduce releaseReduce generationOrganic active ingredientsRespiratory disorderInflammatory factorsPhosphorylation
The invention discloses application of brefeldin A in preparation of an inflammatory factor active inhibitor medicine. It is discovered that the brefeldin A can significantly reduce release of TNF-alpha in MH-S and generation of KC in an MLE-12 cell, significantly improve the pathological change of the lung tissue of a mouse, reduce the content of leucocytes and TNF-alpha in BALF, significantly reduce the activity of MPO in the lung tissue of the mouse, significantly improve the cAMP level and significantly inhibit phosphorylation of ERK. The Brefeldin A can achieve a protection effect on acute lung injuries, and the mechanism of the Brefeldin A may be related to ways of increasing the content of cAMP in cells, inhibiting the phosphorylation of the ERK and the like. According to the application, a new research direction is provided for the therapeutic target of the acute lung injuries, by adjusting protein translocation in the cells, generation and secretion of the inflammatory factormay be inhibited, and therefore development of inflammation is hindered.
Owner:ZHEJIANG UNIV
Brefeldin A ester derivatives and their preparation and application
ActiveCN105153136BImproves antioxidant activityGood antitumor activityOrganic chemistryAntinoxious agentsDiseaseDrug development
The invention discloses brefeldin A ester derivatives, and preparation and application thereof. The brefeldin A ester derivative compounds have antioxidation activity and antitumor activity, wherein the brefeldin A ester derivative compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable antioxidation effect and can remove DPPH, ABTS and super oxygen free radical (O2<->), and the compound (I-7) has better removal effect on DPPH, ABTS and super oxygen free radical (O2<->) than vitamin E; and the compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable inhibition activity for human lung cancer cells A549. Therefore, the result shows that the derivatives have wide application prospects in the drug development system, provide a new and broader idea for synthesizing and screening BFA (brefeldin A) derivative drugs and provide a more efficient way for treating related diseases.
Owner:ZHEJIANG UNIV OF TECH
Brefeldin A ester derivatives and their preparation and application
ActiveCN103788053BSimple methodHigh inhibition rateOrganic active ingredientsOrganic chemistryKidney cancerProstate cancer
The invention provides brefeldin A ester derivatives having antitumor activity and their preparation method and use. The brefeldin A ester derivatives have structures shown in the structural general formula (I). The brefeldin A ester derivatives have high effects on esophagus cancer, lung cancer, kidney cancer, colorectal cancer and prostatic cancer and have an in-vitro detection effective inhibition rate of 80%. The preparation method of the brefeldin A ester derivatives has simple processes and can be operated easily.
Owner:ZHEJIANG UNIV OF TECH
4,7-position melphalan-like nitrogen mustard derivative of brefeldin a, its preparation method and use
ActiveCN110028480BImprove pharmacological activityOrganic active ingredientsOrganic chemistryAlkylating antineoplastic agentPharmaceutical medicine
The invention belongs to the field of natural medicine and medicinal chemistry, and relates to a preparation method and uses of a brefeldin A derivative with melphalan-based chlormethine linked at site 4 and site 7, specifically to a preparation method for introducing DNA alkylating agent melphalan derivatives at the 4-OH site and the 7-OH site of brefeldin A, and applications in preparation of antitumor drugs. According to the present invention, the brefeldin A derivative with melphalan-based chlormethine linked at site 4 and site 7, and the pharmaceutically acceptable salt have a structure represented by a general formula I, wherein n is defined in the claim and specification.
Owner:SHENYANG PHARMA UNIVERSITY
A kind of preparation method and application of 4-position splicing nitrogen mustard derivatives of brefeldin a
ActiveCN110028477BImprove pharmacological activityOrganic active ingredientsOrganic chemistryPharmaceutical drugPharmaceutical medicine
The invention belongs to the field of natural medicine and medicinal chemistry, and relates to a preparation method and uses of a class of brefeldin A derivative containing chlormethine linked at site4 and having antitumor activity, wherein the brefeldin A derivative containing chlormethine linked at site 4, and the pharmaceutically acceptable salt have a structure represented by the following general formula I, and n is defined in the claim and specification.
Owner:SHENYANG PHARMA UNIVERSITY
Application of brefeldin A ester derivative in antitumor drug
The invention relates to the field of medicinal chemistry, and in particular, relates to an application of a brefeldin A ester derivative in the aspect of inhibiting tumor proliferation activity; the brefeldin A ester derivative can be used for preventing or treating hyperproliferative diseases, and the structure of the brefeldin A ester derivative is represented by a formula (I). Hyperproliferative diseases comprise liver cancer, leukemia, breast cancer, colonic adenocarcinoma, gastric cancer, lung cancer, Bartter's esophagus cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymph cancer, kidney cancer, brain cancer, nerve cancer, nasopharynx cancer, oral cancer and colorectal cancer, so that the brefeldin A ester derivative has the potential of being developed into a novel antitumor drug.
Owner:OCEAN UNIV OF CHINA
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