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396 results about "Colonic Cancers" patented technology

Colon cancer lymph node metastasis risk prediction method and system based on image analysis

The invention relates to the field of image analysis, in particular to a colon cancer lymph node metastasis risk prediction method and system based on image analysis. The method comprises the following steps: acquiring a pathological section scanning image, carrying out layer-by-layer downsampling and feature reconstruction, and generating pathological section topological features; carrying out adaptive clustering analysis and multi-parameter fusion evaluation on the basis of the pathological section topological features to obtain independent migration evaluation values of individual tumor cells; performing tumor metastasis branch analysis according to the independent migration evaluation value, and constructing a metastasis branch path distribution diagram; extracting an immunohistochemical staining image of a patient to obtain immune cell space distribution data; and performing multi-region lymphatic metastasis simulation and metastasis risk situation prediction based on the immune cell spatial distribution data and the metastasis branch path distribution diagram to obtain a final metastasis risk assessment result. According to the method, the lymph node metastasis risk is accurately and efficiently analyzed, and the credibility of a pathological analysis result is improved.
Owner:SHENZHEN BAOAN DISTRICT PEOPLES HOSPITAL

Multi-dimensional efficacy evaluation system for colon cancer targeted drug screening

The invention discloses a multi-dimensional efficacy evaluation system for colon cancer targeted drug screening, and relates to the technical field of medical assistance. Comprising a data acquisition module, an inference engine module and an output module. The data acquisition module acquires an organ sample response data set (including apoptosis rate A1, activity decline degree A2 and image structure change score B1) and a patient background data set (including gene mutation discrete variable set G and metabolic pathway continuous variable set M). The inference engine module executes dominant condition rules: generating a negative weight factor alpha according to a gene mutation state and a metabolic activation threshold value; generating a deduction item gamma based on a preset drug-resistant mutation subset; performing weighted calculation on the apoptosis rate and the activity decline degree to generate a basic drug effect score beta, and increasing beta through a critical value; and finally generating a comprehensive response score S. And the output module outputs a drug effect judgment result according to the S, and multi-dimensional accurate evaluation is realized.
Owner:YANBIAN UNIV

Application of combination of target protein circPIAS1-108aa inhibitor and oxaliplatin in preparation of drug synergistic composition for treating cancer

The invention discloses application of a target protein circPIAS1-108aa inhibitor combined with oxaliplatin in preparation of a medicine synergistic composition for treating cancers, the specific action mechanism of circPIAS1-108aa in colon cancer treatment is found for the first time, and further research shows that by using siRNA to knock down circPIAS1-108aa, colon cancer cell proliferation can be remarkably inhibited, and the effect of treating the colon cancer can be achieved. Furthermore, the target spot protein circPIAS1-108aa inhibitor can be used for enhancing the treatment effect of the oxaliplatin. Therefore, when the circPIAS1-108aa expression is inhibited in a targeted manner and the oxaliplatin is combined for use, the circPIAS1-108aa can be obviously used for preventing and treating cancers, the dosage and toxic and side effects of the oxaliplatin are reduced, and a new synergistic strategy is provided for tumor treatment.
Owner:CHINA PHARM UNIV

3-sulfamoyl benzamide compound as well as preparation method and application thereof

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 3-sulfamoyl benzamide compound as well as a preparation method and application thereof. The 3-sulfamoyl benzamide compound has a structure as shown in a formula I. In the formula I, X is chlorine or trifluoromethyl; r1 and R2 are independently C1-4 alkyl or R1, R2 and N atoms connected with R1 and R2 jointly form a heterocyclic group, and the heterocyclic group is a substituted or unsubstituted five-membered or six-membered heterocyclic group; and when the heterocyclic group is a substituted heterocyclic group, the substituent group in the substituted heterocyclic group is one or more of C1-4 alkyl, phenyl and acetyl. The 3-sulfamoyl benzamide compound disclosed by the invention has a remarkable proliferation inhibition effect on HCT116 colon cancer cells, HeLa human cervical cancer cells, MDA-MB-231 human breast cancer cells and A375 human malignant melanoma cells.
Owner:PEKING UNIV

Colon cancer CT image segmentation method and system fusing individualized features

The invention belongs to the field of medical image processing and artificial intelligence, and provides a colon cancer CT image segmentation method and system fusing individualized features, and the method comprises the steps: obtaining the abdomen CT images of a historical patient and a target patient; obtaining structured individual feature information related to the patient, wherein the individual feature information comprises age, gender, colon cancer family history and intestinal medical history information; preprocessing the abdomen CT image; and training an image segmentation model by using the preprocessed abdominal CT image of the historical patient, segmenting the preprocessed abdominal CT image of the target patient by using the trained image segmentation model meeting the segmentation precision requirement, and generating a colon cancer focus segmentation image conforming to the individual feature difference of the target patient. According to the method, the structured patient information is utilized to guide the model network to adjust the feature response, so that the segmentation precision and individual adaptability of the model are improved, and the segmentation accuracy is further improved.
Owner:FUDAN UNIV SHANGHAI CANCER CENT +1

Application of natural compound targeting colon cancer drug resistance related protein

The invention is applicable to the technical field of biological medicines, provides application of a natural compound of a targeted colon cancer drug resistance related protein, and particularly relates to application in preparation of drugs for preventing or treating colon cancer. According to the invention, a natural small molecule compound neohesperidin dihydrochalcone targeting the colon cancer drug resistance related protein TAGLN is screened out, and a new scheme is provided for reversing colon cancer drug resistance, so that the situation that no drug is available to the target spot is solved. Secondly, the invention also provides a scheme for combined use of neohesperidin dihydrochalcone and oxaliplatin, the scheme can significantly enhance the killing effect of oxaliplatin on drug-resistant colon cancer, and a new choice is provided for clinical treatment of colon cancer.
Owner:JILIN UNIVERSITY

A pentacyclic thiazolyl indolinone piperazine amide derivative and uses thereof

PendingCN122444757ACarbamateO-Phosphoric Acid
The present application relates to a kind of five-ring thiazole indole ketone piperazine amide derivatives and purposes thereof.The derivatives take ethyl cyanoacetate as starting material, generate hydroxylamine compound (A) under the action of sodium nitrite and phosphoric acid;Obtain 2-amino ethyl cyanoacetate (B) by reduction, in turn with acetic anhydride, lawson reagent is reacted, and 5-amino-4-carboxylate thiazole compound (D) is obtained;After bromination by NBS, under the catalysis of phosphorus oxychloride, react with tetrahydropyridine indole ketone, generate 2-bromo-6,7-dihydrothiazolo [5'',4'':4',5'] pyrimido [1',2':1,2] pyrindo [3,4-b] indole-4 (12H) -ketone (F), again under alkaline condition, first with Boc piperazine, then by Boc treatment and obtain compound (H);Finally, react with acyl chloride, and 28 different substitution structures of five-ring thiazole indole ketone piperazine amide compound (I1-I28) are synthesized.The 28 compounds are tested on three kinds of cancer cells, and the results show that: 28 compounds have significant inhibitory activity on Hela cervical cancer cells, HT-29 human colon cancer cells and HGC-27 human gastric cancer cells.
Owner:XINJIANG INST OF ENG

TMEM86A targeting siRNA and application thereof

The invention discloses siRNA (small interfering Ribonucleic Acid) targeting TMEM86A and application thereof, and relates to the technical field of biology, the siRNA comprises the following positive-sense strands and antisense strands: siRNA-001: a positive-sense strand: 5 '-GAAGAGCGAAGGACCCAAATT-3'; according to the tumor-associated macrophage, TMEM86A has a positive-sense strand of 5 '-TTTGGGTCCTTCGCTTCT-3', an antisense strand of 5 '-TTTGGGTCCTGTCGCTTCT-3', siRNA-002 has a positive-sense strand of 5 '-GGCTCATGGTTCGGTTTT-3', and an antisense strand of 5 '-AAACCGAACCCATGAGCCT-3'. According to the tumor-associated macrophage, single cell sequencing analysis finds that TMEM86A is highly expressed in tumor-associated macrophages, and the development of tumors is inhibited by designing siRNA of TMEM86A to target the tumor-associated macrophages in a colon cancer tumor microenvironment.
Owner:THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV

Spleen-targeted nano platform construction method suitable for tumor vaccination

The invention discloses a spleen-targeted nano platform construction method suitable for tumor vaccination, and particularly relates to the field of vaccines.The spleen-targeted nano platform construction method comprises the steps that S1, CL15H6-DOPS LNPs, spherical polymer vesicles and erythrocyte membrane coated nano-particles are selected as spleen-targeted nano-carriers; s2, integrating an immunologic adjuvant; mn < 2 + > doped LNPs, ultrasonic response lipidosome and a CD3 antibody are selected to be coupled to serve as an integration material; s3, delivering in vivo; animal models are selected for in-vivo delivery and curative effect verification, and B16F10 melanoma mice, MC38 colon cancer mice and non-human primates are selected as the animal models respectively. By optimizing the chain length and the surface topological structure (such as spherical polymer vesicles) of the liposome, the spleen enrichment rate is remarkably increased, and the red marrow myeloid cell uptake efficiency is enhanced. By combining with common delivery of a manganese adjuvant, an STING channel is activated, secretion of type I interferon is promoted, and the proportion of antigen-specific CD8 + T cells and the tumor inhibition rate are increased.
Owner:UNIV OF SCI & TECH OF CHINA

CXCL6-targeting blocking antibody and application thereof in preparation of antitumor drugs

The invention relates to the technical field of biological medicines, and discloses a blocking antibody targeting CXCL6 and an application of the blocking antibody in preparation of antitumor drugs. The antibody or antigen-binding fragment thereof is capable of binding specifically to human CXCL6 protein with high affinity (e.g., Kd < = 1 nM). According to the invention, the specificity and high affinity of the antibody are verified by Western Blot, immunofluorescence, immunohistochemistry and surface plasmon resonance (SPR) technologies. Functional experiments show that the antibody can effectively block CXCL6-induced neutrophil chemotaxis, including in Transwell, a three-dimensional gel model and a zebra fish living body model. Besides, in a mouse MC38 colon cancer model, the antibody shows remarkable anti-tumor activity and can inhibit tumor growth driven by CXCL6. The invention also provides a pharmaceutical composition containing the antibody, and application of the antibody in preparation of drugs for preventing or treating diseases (such as inflammatory diseases, autoimmune diseases and cancers) related to abnormal expression or activity of CXCL6.
Owner:AFFILIATED HOSPITAL OF JINING MEDICAL UNIV

Three-specificity immune cell adapter-cytokine fusion protein, and preparation method and application thereof

The invention provides a three-specificity immune cell adapter-cytokine fusion protein for malignant tumor immunotherapy as well as a preparation method and application of the three-specificity immune cell adapter-cytokine fusion protein. The fusion protein comprises a first binding domain, a second binding domain and a cytokine structural domain which are covalently linked to form a single polypeptide chain or polypeptide compound. The first binding domain is specifically bound with a tumor associated antigen, and the target spot of the first binding domain comprises but is not limited to KK-LC-1, MSLN, HER2, Claudin18.2, Claudin6 and PSMA; the second binding domain is specifically bound with a CD3 protein complex on the surface of the T cell; the cytokine domain is IL2, IL15, IL12, IL21 or a functional variant thereof. The invention also relates to a nucleic acid molecule for coding the fusion protein, an expression vector and application thereof. The fusion protein can be used for immunotherapy of malignant tumors such as colon cancer, gastric cancer, breast cancer, liver cancer, lung cancer and cervical cancer, and has a good application prospect. The invention effectively solves the problems of insufficient T cell activation and limited killing in solid tumor immunotherapy in the prior art.
Owner:NANJING DRUM TOWER HOSPITAL

Use of natural compounds targeting colon cancer drug resistance associated proteins

The application belongs to the technical field of biological medicine, and provides application of a natural compound targeting colon cancer drug resistance related protein, in particular, application in preparation of a drug for preventing or treating colon cancer; the application screens out a natural small-molecule compound hesperetin dihydrochalcone targeting colon cancer drug resistance related protein TAGLN, and provides a new scheme for reversing colon cancer drug resistance, so as to solve the situation that no drug is available for the target point. In addition, the application further provides a scheme in which hesperetin dihydrochalcone is combined with oxaliplatin, and the scheme can significantly enhance the killing effect of oxaliplatin on drug-resistant colon cancer, thereby providing a new choice for clinical treatment of colon cancer.
Owner:JILIN UNIVERSITY

Antibody-drug conjugates and preparation methods and use thereof

The present application relates to an antibody-drug conjugate and its preparation methods and use, and specifically relates to an antibody-drug conjugate for treating HER3-positive cancers. The present application provides a fully human HER3 antibody, which has excellent binding activity to HER3-positive cells and can efficiently deliver drugs to HER3-positive cells. The present application also provides a drug-linker molecule coupled to the antibody, and the drug comprises a DNA topoisomerase inhibitor. The obtained antibody-drug conjugate has a better drug-to-antibody ratio, and has a good targeted killing effect on colon cancer, gastric cancer, breast cancer, and lung cancer (e.g., non-small cell lung cancer, specifically, lung adenocarcinoma). Therefore, the present application further provides a preparation method for the antibody-drug conjugate and application of the antibody-drug conjugate in the treatment of a HER3-positive cancer.
Owner:SICHUAN KELUN BIOTECH BIOPHARMACEUTICAL CO LTD

Methods of treatment

The disclosure relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) useful for the treatment of certain cancers or tumors, such as colon cancer. In another embodiment, the disclosure relates to the use of inhibitors of PDE1 and an optional antitumor agent for the treatment of certain cancers or tumors.
Owner:INTRA CELLULAR THERAPIES INC

Compound containing artemisinin similar structure and application thereof

The invention discloses a compound containing an artemisinin similar structure or a pharmaceutical salt thereof, and the structural general formula is as follows: # imgabs0. The compound containing the artemisinin similar structure, provided by the invention, has a relatively obvious proliferation inhibition effect on solid tumor cells such as lung cancer A549, colon cancer HCT116 and liver cancer HepG2; wherein the high-activity compound has an excellent proliferation inhibition effect on leukemia cells HL-60 and MV4-11, is better than a marketed drug SAHA, and can be used as an anti-tumor candidate drug for deeper research.
Owner:FOURTH MILITARY MEDICAL UNIVERSITY +1

Preparation of methoxyl derivative and application of methoxyl derivative in pharmacy

The invention discloses preparation of a methoxyl derivative and application of the methoxyl derivative in pharmacy. The methoxy derivative as shown in the formula I has good anti-tumor activity, and the anti-tumor effect is effectively achieved through the growth inhibition and killing effect on tumor cells. The methoxyl derivative not only can inhibit the growth of CT26 transplanted tumors, but also can promote the activation and infiltration of lymphocytes in an in-vivo tumor microenvironment. Meanwhile, the compound also has a remarkable inhibiting effect on the growth of mouse colon cancer CT26 cell strains in vitro.
Owner:成都市第一人民医院

Automatic tumor region labeling method for whole slide pathological images of colon cancer

This invention discloses an automatic tumor region annotation method for whole-section pathological images of colorectal cancer, belonging to the field of pathological image processing technology. It employs an improved Inception-V3 network, embedding a colorectal cancer feature extraction branch to extract cellular, glandular, and tissue-level morphological features associated with colorectal cancer from stained whole-section pathological images. A fused feature map is obtained by weighting the contribution coefficients of colorectal cancer gene morphology. Based on the colorectal cancer morphological fingerprint vector, an improved Otsu algorithm is used to generate an initial segmentation threshold. The optimal segmentation threshold is obtained through iterative optimization using a colorectal cancer gene morphology matching degree formula, thus initially dividing the tumor candidate region. This invention deeply couples the molecular features of core driver mutation genes in colorectal cancer with the morphological features of pathological images, constructing a dedicated morphological fingerprint database for gene-morphology coupling. This ensures that tumor region annotation aligns with the clinical diagnostic criteria combining molecular and histopathological aspects of colorectal cancer, improving the clinical adaptability of the annotation results.
Owner:RENMIN HOSPITAL OF WUHAN UNIVERSITY (HUBEI GENERAL HOSPITAL)

Antibody-drug conjugates, their production methods, and uses

The present application relates to an antibody-drug conjugate, a method for producing the same, and uses thereof. Specifically, the present application relates to an antibody-drug conjugate for use in treating B7-H3-positive tumors. The antibody-drug conjugate of the present application comprises a B7-H3 antibody, which has excellent binding activity to B7-H3-positive cells and can efficiently transport drugs to B7-H3-positive cells. The antibody-drug conjugate of the present application has an excellent drug-antibody binding ratio and exhibits excellent targeted killing effects against tumors such as lung cancer, breast cancer, gastric cancer, and colon cancer. Therefore, the present application further provides a method for producing the antibody-drug conjugate and its use in treating B7-H3-positive tumors.
Owner:SUCHUAN KORN - BIOTECH BIOPHARMACEUTICAL CO LTD

Musa basjoo root extract and application thereof in preparation of antitumor drugs

The invention belongs to the technical field of medicines, and particularly relates to a Japanese banana root extract and application thereof in preparation of antitumor drugs, and a preparation method of the Japanese banana root extract comprises the following steps: 1) raw material pretreatment; 2) extracting; (3) concentrating and purifying; and 4) extracting and drying. The Japanese banana root extract shows broad-spectrum activity in the anti-tumor aspect, in-vitro experimental data shows that the Japanese banana root extract has an inhibiting effect on various tumors such as cervical cancer, triple negative breast cancer, lung cancer, liver cancer and colon cancer, and in addition, the Japanese banana root extract can be used as a chemotherapy sensitizer and has multiple application values in tumor comprehensive treatment.
Owner:GUANGXI JIULV PHARM CO LTD

Naphthopyrimidino-fused heteroazasugar derivatives, methods of synthesis and use thereof

This invention provides a naphthopyrimidine-fused-acid sugar derivative, its synthesis method, and its application, belonging to the field of pharmaceutical technology. The naphthopyrimidine-fused-acid sugar derivative has the structures shown in formulas (I) to (IV). These compounds are obtained by one-step cyclization via a condensation reaction with 1,8-diaminonaphthalene in an organic solvent under the catalysis of a trifluoromethanesulfonate catalyst, using a propionyl-protected and p-toluenesulfonated sugar as the starting material. The preparation method is efficient and simple. The compounds of this invention exhibit good anti-proliferative activity against colon cancer tumor cells.
Owner:HEBEI UNIVERSITY

An intestinal microbiota Bacteroides fragilis toxin-neutralizing nanobody and its application

The present invention discloses an intestinal microbiota Bacteroides fragilis toxin-neutralizing nanobody and its application. By deeply studying the enterotoxigenic Bacteroides fragilis and the toxin BFT secreted by it in the bodies of patients with colorectal cancer and breast cancer, nanobodies against BFT are expressed by phage display technology; nanobodies with high binding affinity to the antigen are screened out through biopanning technology; a nanobody with the ability to neutralize the toxicity of BFT, also known as Nb2.43, is obtained. The present invention expresses and optimizes to obtain a BFT nanobody protein with high affinity, stability and uniformity, opening up a new field for the treatment of colorectal cancer and breast cancer with nanobodies targeting BFT, and having good research value and application prospects.
Owner:THE FIRST AFFILIATED HOSPITAL OF MEDICAL COLLEGE OF XIAN JIAOTONG UNIV +1

A shRNA targeting and inhibiting MZF1 gene expression and its application

The present invention relates to the field of genetic engineering technology, specifically to a shRNA for targeted inhibition of MZF1 gene expression and its use. The shRNA's target sequence is selected from the nucleotide sequence set forth in SEQ ID NO: 1 or SEQ ID NO: 2. The shRNA is capable of sustained, stable, efficient, and specific inhibition of MZF1 gene expression, providing a highly specific, stable, and reliable new strategy for gene therapy of colon cancer.
Owner:NANJING GENERAL HOSPITAL NANJING MILLITARY COMMAND P L A

Enteric cavity inner segment filling controllable device for T stage before colon cancer operation

The invention relates to the technical field of medical instruments, in particular to an enteric cavity segment filling controllable device for colon cancer preoperative T staging, which comprises a central mandrel, a flexible head end cap is arranged at the foremost end of the central mandrel, and a near-end balloon inflating pipeline, a far-end balloon inflating pipeline and a main pipeline which are mutually independent are arranged in the central mandrel; the near-end balloon is arranged on the central mandrel in a sleeving manner and is communicated with the near-end balloon inflating pipeline; the far-end balloon is arranged on the central mandrel in a sleeving manner, is positioned on the far side of the near-end balloon and is communicated with the far-end balloon inflating pipeline; at least two main pipeline lateral holes are formed in the tube wall of the central mandrel between the near-end balloon and the far-end balloon, are communicated with the main pipeline and are used for injecting a contrast agent or normal saline into the closed enteric cavity section between the two balloons. The near-end balloon and the far-end balloon are synchronously filled at the two ends of a target intestinal segment to form a closed segment, and a contrast agent is uniformly injected through lateral opening, so that the intestinal wall is fully expanded and does not collapse, and the display definition of the five-layer structure of the intestinal wall is remarkably improved.
Owner:AFFILIATED ZHONGSHAN HOSPITAL OF DALIAN UNIV

Compounds for selective binding to estrogen receptors alpha / beta relative to GPER / GPR30 and methods of treating disease states and conditions mediated through these receptors

The current invention is in the field of molecular biology / pharmacology and provides novel 3-oxabicyclo[3.3.1]nonene compounds and derivatives that modulate the effects of the classical estrogen receptors alpha and beta (ERalpha and ERbeta) with little to no biological or physiological effects on the G protein-coupled estrogen receptor GPER (also known as GPR30). These compounds may function as agonists and / or antagonists of one or more of the disclosed classical estrogen receptors. Diseases that are mediated through one or more of these receptors include cancer (including but not limited to breast (particularly endocrine or anti-hormone resistant, and for the prevention / reduction of endocrine or anti-hormone resistance), reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometritis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disorders (such as Parkinson's disease and Alzheimer's disease), as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine, among numerous others as described herein. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.
Owner:ARROWHEAD CENTER INC +1

Method and system for screening colon cancer diagnosis markers based on transcriptome data

PendingCN121460122AMedical automated diagnosisBioinformaticsCancers diagnosisDiagnostic Specificity
The invention discloses a colon cancer diagnostic marker screening method and system based on transcriptome data, and belongs to the technical field of biological information, and the method comprises the steps of data preparation, pathological hierarchical modeling, diagnostic marker screening and screening report generation. According to the method, pathological hierarchical modeling based on dynamic discrimination and double-layer feature fusion is adopted, on the basis of comprehensively considering gene expression and pathological morphology information, pathological subtypes of colon cancer samples are adaptively recognized, stable and representative subtype features are obtained, and therefore the accuracy and biological representativeness of diagnostic marker screening are improved; diagnostic marker screening based on pathological subtype difference analysis is adopted, and on the premise of considering pathological subtype characteristics, a stable and reliable diagnostic marker set with remarkable expression difference is screened in a targeted manner, so that the biological representativeness, screening robustness and diagnostic specificity of markers are improved.
Owner:固原市人民医院

Tricyclic heterocyclic compound as well as preparation method and medical application thereof

The invention relates to a tricyclic heterocyclic compound as well as a preparation method and medical application thereof. Specifically, the invention relates to a compound shown in a general formula (I), a preparation method of the compound, a pharmaceutical composition containing the compound and application of the compound as an MAT2A inhibitor. The compound and the pharmaceutical composition containing the compound can be used for treating and / or preventing diseases related to MAT2A activity, such as mesothelioma, neuroblastoma, rectal cancer, colon cancer, esophageal cancer and the like. Wherein the definition of each group in the general formula (I) is the same as that in the specification.
Owner:CHINA RESOURCES PHARM RES INST (SHENZHEN) CO LTD

Sporosporine glycoside derivative as well as preparation method and application thereof

The invention discloses a staurosporine glucoside derivative as well as a preparation method and application thereof, and belongs to the field of medicine synthesis. C3-NHCH3 of staurosporine is subjected to glycosylation modification, and the staurosporine glycoside derivative shown in the formula (I) is prepared. The glycoside derivative prepared by the invention has a better inhibition effect on human acute myeloid leukemia cells THP-1, human bladder cancer cells 5637, human colon cancer cells HCT-116, human pancreatic cancer cells PATU8988T and human liver cancer cells HuH-7, and the compound 5 also has an excellent inhibition effect on human gastric cancer cells MKN-45. A candidate compound is provided for development of drugs for bladder cancer, colon cancer, pancreatic cancer, liver cancer, stomach cancer or acute myeloid leukemia.
Owner:OCEAN UNIV OF CHINA