570 results about "Lead compound" patented technology

The invention belongs to the field of bioinformatics, and relates to a molecular property prediction method based on multi-modal gating and comparative learning, which comprises the technologies of comparative learning, graph neural network, cross-modal alignment, gating attention and the like. Firstly, data standardization and graph construction are carried out, and molecular fingerprint embedding is extracted; secondly, a heterogeneous dual-channel graph coding architecture is adopted, one path captures atom short-range interaction through an attention mechanism, the other path integrates a molecular global structure and long-range dependence, and complementary molecular representation is generated; then, a cross-modal attention mechanism is introduced, bidirectional association of graph and fingerprint features is achieved, and modal weights are adaptively and dynamically distributed through a gating fusion module; and finally, a comparison pre-training strategy is adopted, a molecular graph and fingerprints are utilized to construct a sample pair, and discriminative molecular representation is learned on unlabeled data. According to the method, the accuracy of molecular property prediction is remarkably improved, and an efficient and reliable calculation tool is provided for virtual drug screening and lead compound optimization.

The invention is applicable to the technical field of drug research and development, and provides a lead compound discovery method based on a large language model, which comprises the following steps: determining a target spot and constructing an initial compound library; generating fragments and forming an initial fragment library; calculating the frequency of occurrence of the fragments and the affinity contribution degree of the fragments to the target protein, and updating the fragment library; fragment sampling weight calculation and candidate fragment selection; the large language model generates molecules according to the candidate fragments; evaluating the quality of the generated molecules and updating the molecule library; and repeating the cycle until a preset iteration round number is reached. A fragment-based drug design method is combined with the large language model, rich domain knowledge of the large language model is used for replacing human experts to guide drug design, fragments are used as prompts to stimulate the internal potential of the large language model, the advantages of the two methods complement each other, exploration of the whole chemical space is completed, and the drug design efficiency is improved. The lead compound reaching the human expert level is designed in actual use, and a new technical means is provided for drug research and development.

The invention discloses a hexapeptide with a hypoglycemic effect as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The amino acid sequence of the hexapeptide is Ile-Trp-Asp-Pro-His-Phe, and the amino acid sequence of the hexapeptide is as shown in the specification. The novel hexapeptide IWDPHF with prominent DPP-IV inhibition ability is successfully identified from mulberry leaf proteolysis products through liquid chromatography-mass spectrometry and a virtual screening method, the hexapeptide IWDPHF shows the blood glucose reducing effect superior to that of part of known peptides in an in-vitro enzyme activity inhibition experiment and a zebra fish hyperglycemia model, and no obvious side effect exists; the compound has a good potential of being developed into a hypoglycemic functional product or a drug lead compound. The invention further provides the mulberry leaf peptide with the peptide fragment IWDPHF, and the mulberry leaf peptide can be applied to preparation of drugs or food for reducing blood sugar. The invention provides a new scheme and theoretical basis for treatment of diabetes, and has good market prospect and application potential.

The present invention discloses the application of a 1,7-dihydro-6H-purin-6-one compound in the preparation of an anti-pulmonary fibrosis drug, which relates to the technical field of biomedicine. The application of the 1,7-dihydro-6H-purin-6-one compound of the present invention in the preparation of an anti-pulmonary fibrosis drug detects the anti-pulmonary fibrosis pharmacological activity of the 1,7-dihydro-6H-purin-6-one compound after structural modification and transformation, tests the pharmacological activity of this type of compound in a variety of animal disease models, and provides data on the activity of preventing and treating different types of pulmonary fibrosis, confirming that they all have good activity, and the effect is significantly better than the clinically commonly used positive drug nintedanib, and the effect is also better than hypoxanthine analogs A, B, and C. The application of the 1,7-dihydro-6H-purin-6-one compound of the present invention in the preparation of an anti-pulmonary fibrosis drug can provide a new skeleton for the screening of new compounds for the preparation of anti-pulmonary fibrosis drugs, and lay a theoretical foundation for the development of new lead compounds.

The invention discloses pancreatic lipase immobilized composite nano magnetic beads, a preparation method and application, ferroferric oxide is adopted as a magnetic core, dopamine-mediated growth is performed to form a core-shell structure, then the periphery of the core-shell structure is wrapped with a metal organic framework to form the composite nano magnetic beads, and pancreatic lipase is immobilized by using the composite nano magnetic beads as an adsorption carrier. The enzyme loading amount, the repeated utilization rate and the storage stability of the ferroferric oxide nano-particles are remarkably improved, the enzyme immobilization efficiency and the enzyme activity are improved, and meanwhile, the prepared pancreatic lipase immobilized composite nano-magnetic beads have excellent stability and biocompatibility, are green and pollution-free and can be repeatedly used; the composite nano magnetic beads are synthesized by adopting a solvothermal method, the product is easy to separate, the synthesis process is simple, the enzyme immobilization efficiency can be regulated and controlled by regulating and controlling the synthesis process, the structure of an active ligand can be screened and analyzed from natural products with numerous and jumbled components, and the active ligand has a certain lipid-lowering potential and can be used for preparing the nano magnetic beads. The compound can be used as a potential lead compound of lipid-lowering drugs.

The present disclosure relates to novel small molecules, particularly, sulforaphane analogues (SFNAs) as well as αCD / SFNAs inclusion complexes and their use as lead compounds for manufacturing a medicament or a pharmaceutical composition for therapy, in particular, for treating cancer.

The present invention discloses a culture medium, a fermentation method and an application of Streptomyces for producing pieridian glycosides. Through this fermentation method, the Streptomyces can produce abundant pieridian glycosides, and its effective part contains more than 8 types of pieridian glycosides at the same time, and the content of the four types of pieridian glycosides, namely compound 4, compound 5, compound 6 and compound 8, is greater than 5%. The extract obtained by the strain through this fermentation method and its effective part can be used to prepare drug lead compounds for treating renal cancer, organ fibrosis, acute kidney injury and chronic kidney disease, and can provide drug source guarantee for China's marine drug research and development.

The invention discloses a novel benzofuran component in eupatorium chinense and application of the benzofuran component in anti-inflammatory activity. The obtained compound is separated from an eupatorium chinense extract. The eupatorium chinense root extract is separated by using an extraction method, macroporous adsorption resin impurity removal, Sephadex LH-20 gel column chromatography, high performance liquid chromatography and other methods. According to the present invention, all the separated compounds and the analogues thereof have good inhibition activity on target cyclooxygenase-2 of inflammation-related diseases, and have good inhibition activity on COX-2 enzyme, and the molecular docking experiment results show that the compounds and the target proteins have good binding energy. Therefore, the compound can be used for preparing drugs for treating inflammatory related diseases, or anti-inflammatory and analgesic drugs, or tumor drugs by inhibiting COX-2 enzyme, such as drugs for rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, Alzheimer's disease and the like, and related natural lead compounds are provided.

The invention discloses a lead compound optimization method and system based on skeleton constraint and training enhancement, and belongs to the field of artificial intelligence drug discovery. The method comprises the following steps: performing structural treatment on an initial lead compound, extracting a growth skeleton structure, and pairing a protein pocket structure; inputting information of the skeleton structure and the protein pocket structure into a coding model based on a three-dimensional graph neural network for joint coding to obtain structure coding representation; on the basis of a Delete model, an atomic distance-based resampling mechanism and a hydrophobic group mask are introduced, and a molecular generation model is constructed; training and tuning a molecule generation model through staged pre-training and a knowledge enhancement fine tuning strategy so as to improve the structural accuracy, the binding activity and the druggability of generated molecules; and inputting the structure coding expression into a trained and optimized molecular generation model PocketGrow to generate optimized molecules, screening the generated optimized molecules, and outputting a lead compound with development potential.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 2-aminopyrimidine compound, application thereof and an antitumor drug. The 2-aminopyrimidine compound provided by the invention has a structure as shown in a formula (I). According to the invention, 2-aminopyrimidine is used as a mother nucleus structure, and a series of 2-aminopyrimidine compounds are successfully constructed by accurately introducing a biologically active imidazole, thiazole or oxazole nitrogen-containing heterocyclic ring fragment at the 5 # site of 2-aminopyrimidine; systematic in-vitro anti-tumor activity evaluation proves that the 2-aminopyrimidine compound with the structure as shown in the formula (I) provided by the invention shows remarkable inhibitory activity on various tumor cell lines, and the activity of part of the compound is even superior to that of a clinical control drug. The structural diversity of 2-aminopyrimidine compounds is enriched, valuable lead compounds are provided for developing novel efficient antitumor drugs, and the 2-aminopyrimidine compounds have important scientific significance and clinical transformation potential. # imgabs0 #

The invention belongs to the technical field of biological medicines, and discloses application of beta-elemonic acid or derivatives thereof or pharmaceutically acceptable salts thereof in preparation of medicines for preventing and / or treating polycystic ovarian syndrome (PCOS). The beta-elemonic acid is screened from a medicinal and edible library, and experiments prove that the beta-elemonic acid can remarkably improve the PCOS ovarian form and the number of mature follicles, normalize the disordered estrus cycle, remarkably improve the serum hormone level and further remarkably improve the sugar tolerance, insulin tolerance and weight of PCOS. The beta-elemonic acid disclosed by the invention is a compound based on homology of medicine and food, can be used as a medicine as well as a natural ingredient of food, is relatively low in toxicity, ensures the safety after long-term use, is relatively low in safety evaluation cost of a relatively brand-new synthetic compound, and can be applied to development and preparation of a medicine or a lead compound thereof for preventing and / or treating PCOS, or a health care product.

The invention provides a coumarin derivative containing oxadiazole (thiadiazole) thioether and a preparation method and application thereof, the structural general formula of the coumarin derivative containing oxadiazole (thiadiazole) thioether is shown as I, and the structural general formula of the coumarin derivative containing thiadiazole thioether is shown as II, the synthesis route of the coumarin derivative containing oxadiazole (thiadiazole) thioether is simple and practical, the preparation raw materials are easy to obtain, the cost is low, and the prepared compound has a good control effect on plant viruses including tobacco mosaic virus, cucumber mosaic virus, potato Y virus, southern rice black-streaked dwarf virus or rice stripe virus. According to the invention, a favorable lead compound is provided for the creation of a natural bionic antiviral agent; # imgabs0 #

The invention discloses a multi-target joint optimized antibiotic molecule design system and method applied to the field of biological medicine, and the method comprises the steps: obtaining FabI enzyme and AcrAB-TolC efflux pump structure data, extracting double-target space and physicochemical characteristics, and constructing a joint pharmacophore model containing a FabI inhibition domain and an efflux pump blocking domain; screening candidate molecules meeting a double-domain space matching threshold, screening high-affinity double-target molecules through conformation sampling and free energy calculation, and forming a lead compound library through multi-layer filtration of metabolic stability, membrane penetrability, quantum chemical properties and synthesis feasibility; carrying out electron effect, chain length or heteroatom fine tuning on dominant molecules through in-vitro bacteriostasis and efflux inhibition experiment feedback, and carrying out iterative optimization until MIClt is met; 2 [mu] g / mL and the efflux inhibition rate is gt; according to the present invention, the antibacterial effect and the drug resistance inhibition ability are significantly improved, the molecular synthesizability and the biological safety are ensured, and the engineering design new path is provided for the Gram-negative bacterium drug resistance crisis.

The invention belongs to the technical field of agricultural chemistry, and particularly relates to a naphthoquinone compound with tobacco black shank resisting activity as well as a preparation method and application of the naphthoquinone compound. The naphthoquinone compound is prepared by the following steps: by taking honeysuckle branches as raw materials, extracting with high-concentration methanol, high-concentration acetone / water or high-concentration ethanol / water, merging extracting solutions, filtering, and concentrating under reduced pressure to obtain extract; packing the extract by using a silica gel dry method and carrying out silica gel column chromatography; carrying out gradient elution by using a chloroform-acetone solution; and further separating and purifying the 7: 3 part of the eluent by high performance liquid chromatography to obtain the required naphthoquinone compound. The invention further discloses application of the compound, and activity tests show that the compound has a good inhibiting effect on tobacco black shank. The compound disclosed by the invention is novel in structure, has relatively good black shank resisting activity, can be used as a lead compound for resisting tobacco black shank, and is used for research and development of biological pesticides for preventing and treating tobacco black shank.

The invention discloses a preparation method and application of a benzofuran component in eupatorium chinense. The benzofuran component is separated from an eupatorium chinense extract. The eupatorium chinense root extract is separated by using an extraction method, macroporous adsorption resin impurity removal, HW-40F gel column chromatography, high performance liquid chromatography and other methods to obtain the benzofuran compound. According to the present invention, the inhibition activity of the separated compound on the diabetes-related target alpha-glucosidase is tested, the experimental result shows that the compound has good inhibition activity on the alpha-glucosidase, and the molecular docking experiment shows that the compound has good binding energy with the target protein alpha-glucosidase. Therefore, the compound can be used for preparing drugs for preventing, delaying or treating alpha-glucosidase diseases, especially type II diabetes and obesity, or can be used as a lead compound of the drugs.

The invention discloses a virtual screening method based on a Kv1.3 inhibitor, a drug lead compound and application, and relates to the field of pharmaceutical chemistry. The virtual screening method comprises the following steps: selection and pretreatment of a Kv1.3 protein crystal structure: obtaining a Kv1.3 protein-small molecule compound crystal structure from a Protein Data Bank database, and carrying out pretreatment on the Kv1.3 protein-small molecule compound crystal structure; determining a butt-joint active pocket; selecting a binding site; selecting and downloading a to-be-screened compound library; and virtual screening of the compounds: performing molecular docking by using virtual screening software to obtain the compounds of which the binding free energy (delta G) is negative and the absolute values are ranked from large to small. The compound Z239529546 has the beneficial effects that the compound Z239529546 screened by the method can reduce the expression of related inflammatory factors such as IL-6, IL-1beta, TNF-alpha and the like in cells and Kv1.3 protein in cell experiments, and has a certain effect of treating and / or preventing inflammation.

The invention relates to a 5, 9-di-tert-butyl naphtho-indolizine phenothiazine compound as well as a preparation method and medical application thereof. The compound is efficiently synthesized through Ullmann coupling and palladium-catalyzed intramolecular arylation reaction. In-vitro anti-tumor activity research shows that the compound has remarkable selective inhibitory activity on various human tumor cell lines, and particularly, the inhibitory effect on non-small cell lung cancer A549 cells (IC50 = 0.21 mu M) is improved by two orders of magnitude compared with that of cis-platinum; iC50 (half maximal inhibitory concentration) of other cell lines are as follows: 1.26 mu M of prostate cancer PC-3 cells, 6.78 mu M of liver cancer HepG2 cells, 7.99 mu M of cervical cancer Hela cells and 25.46 mu M of breast cancer MCF-7 cells. Preliminary toxicity experiments prove that the compound has the characteristic of low cytotoxicity. The compound can be used as a novel high-efficiency low-toxicity anti-tumor lead compound, and provides an important structural basis for the development of anti-cancer drugs.

The invention relates to the technical field of biological medicines, in particular to a polycyclic polyisopentenyl cyclopentanone compound as well as a preparation method and application thereof. The polycyclic polyisopentenyl cyclopentanone compound provided by the invention has a structural formula as shown in a formula 1; the preparation method comprises the following steps: by taking dry fruits of hypericum berry as raw materials, carrying out percolation extraction and concentration to obtain an extract, suspending the extract in water to obtain a suspension, and extracting and concentrating the suspension with petroleum ether to obtain a crude extract; the crude extract is taken and subjected to positive and negative phase silica gel column separation, MCI medium-pressure column chromatography, Sephadex LH-20 gel column chromatographic separation, high performance liquid chromatography preparation and CHIRALPAK IG chiral column resolution, and the polycyclic polyisopentenyl cyclopentanone compound is obtained. The protection activity of the compound on AC16 myocardial cell injury induced by cold ischemia is evaluated, and the compound can be used for preparing the polycyclic polyisopentenyl cyclopentanone compound. The compounds can be used as lead compounds for developing medicines for preventing and treating myocardial cold ischemia injury.

The invention discloses application of benzofuran components in eupatorium chinense to reduction of uric acid, compounds 1-3 are obtained by being separated from an eupatorium chinense extract, and the compound 1 is a new compound. The eupatorium chinense root extract is separated by using an extraction method, macroporous adsorption resin impurity removal, HW-40F gel column chromatography, high performance liquid chromatography and other methods to obtain the benzofuran compound. According to the present invention, the inhibition activity of the gout disease related target xanthine oxidase of the separated compound 1-3 is tested, the experimental result shows that the compound 1-3 has good inhibition activity on the xanthine oxidase, and the molecular docking experiment shows that the compound 1-3 has good binding energy with the target protein. Therefore, the compounds 1-3 can be used for preparing a natural lead compound for delaying or treating diseases caused by xanthine oxidase and providing a natural lead compound in the field of treatment of hyperuricemia and gout.

The invention discloses a yunaconitine derivative and application of the yunaconitine derivative in preparation of hypoglycemic and antioxidant drugs, the yunaconitine derivative has a chemical structure as shown in a formula 1a or 1b, and the invention further provides application of the yunaconitine derivative in preparation of PTP1B inhibitors. The dosage form of the medicine is selected from at least one of a tablet, a capsule, a granule, a dripping pill, a suspension, syrup, an enteric-coated preparation, an emulsion suspension and an injection. The yunaconitine derivative disclosed by the invention is high in bioavailability and clinical use value, provides a candidate lead compound for research and development of novel preparations of hypoglycemic and antioxidant drugs, and has potential application value in the fields of hypoglycemic and antioxidant targeted drugs, probe design and fluorescent biomarkers.

The application discloses five-membered sulfur-containing heterocyclic nucleoside leading compounds and application thereof in anti-hand-foot-mouth-disease virus active drugs, and belongs to the technical field of medicinal chemistry. A series of five-membered sulfur-containing heterocyclic nucleoside compounds are synthesized through Sulfa-Michael / Aldol tandem reaction. Results show that in anti-EV-A71 virus testing, the five-membered sulfur-containing heterocyclic nucleoside leading compounds 33a, 5b and 30b have relatively good anti-EV-A71 virus activity, and new structural units are provided for candidate drug molecules for anti-virus.

The invention discloses an anthraquinone compound with anti-MTV activity and a preparation method and application thereof.The anthraquinone compound with the anti-MTV activity is prepared from stems and leaves of desmodium caudatum through the steps of pretreatment, extract extraction, silica gel column chromatography and separation and purification, the molecular formula of the anthraquinone compound with the anti-MTV activity is C18H17O7, and the structural formula of the anthraquinone compound with the anti-MTV activity is shown in the description. The preparation method comprises the following steps: 1, 6-dihydroxy-2, 7, 8-trimethoxy-3-methyl anthracene-9, 10-diketone is used as a raw material, and is named as 1, 6-dihydroxy-2, 7, 8-trimethoxy-3-methyl According to the invention, the English name is 1, 6-dihydroxy-2, 7, 8-trimesoxy-3-methylanthracene-9, 10-dione, and the English name is 1, 6-dihydroxy-2, 7, 8-trimesoxy-3-methylanthracene-9, 10-dione. The present invention has the following structure. Activity tests show that the compound has a certain inhibition effect on MTV. The novel compound disclosed by the invention is novel in structure, has certain anti-MTV activity, can be used as an anti-MTV lead compound, and can be used for research and development of anti-MTV prevention and treatment drugs.

The invention belongs to the field of organic synthesis and medicinal chemistry, and particularly provides an efficient synthesis method of an N, N-diphenyl aniline compound based on a naphtho-indolizino-phenothiazine skeleton and anti-tumor application of the N, N-diphenyl aniline compound based on the naphtho-indolizino-phenothiazine skeleton. Through Suzuki reaction, functional coupling based on a naphtho-indolizino-phenothiazine skeleton and an N, N-diphenyl aniline group is realized for the first time. In-vitro anti-tumor evaluation shows that the compound has remarkable inhibitory activity on various human tumor cells, especially has the strongest effect on breast cancer MCF-7 cells (IC50 = 0.15 mu M), and the activity is improved by 266 times compared with that of cis-platinum; prostate cancer PC-3, liver cancer HepG2, lung adenocarcinoma A549 and cervical cancer Hela cells are also remarkably inhibited. The toxicity to normal umbilical vein endothelial cells (HUVEC) is far lower than that of tumor cells, and the selectivity is excellent. The research provides a lead compound with great potential for developing high-efficiency and low-toxicity targeted anti-tumor drugs.

The invention relates to a plant vaccine lead compound based on carbohydrates and a synthesis method thereof, glucosamine groups are modified by an organic synthesis process, and a derivative with a tetrasaccharide structure, namely a compound 12, with induction activity is obtained by a glycosylation reaction. And then removing part of functional groups to obtain a chitosan oligosaccharide analogue with a clear structure and a single component, namely a compound 14. Through experimental research, optimization of a technology for inducing plant disease resistance by the chitosan oligosaccharide is realized. Results show that the plant vaccine lead compound provided by the invention can obviously promote the growth and development of plants at a lower concentration, so that the product provided by the invention has a good popularization and application prospect in the related field of agriculture.

The invention discloses a phenyl-substituted pyrazolopyridine compound as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The structure of the compound is as follows: # imgabs 0 #, wherein R1 is any one of the following structures: # imgabs 1 #; and R2 is any one of the following structures: # imgabs2. The compound has the beneficial effects that the compound has a proliferation inhibition effect on various tumor cells and can selectively inhibit proliferation of triple negative breast cancer cells MDA-MB-468, the half inhibitory concentration IC50 of the compound 8 is 2.500 M, the selection index SI is 8.428, and the compound 8 can be deeply developed as a lead compound for resisting triple negative breast cancer.

The application discloses a kind of miraculin compounds and its extraction method and application, belong to the field of traditional Chinese medicine extraction, specifically related to a kind of miraculin compounds as shown in general formula (I) and (II) isolated from Rhododendron dauricum and the extraction method of the compound, and the compound or the isomer of the compound, or the inhibitory effect of the compound on inflammation in pharmaceutically acceptable salt or pharmaceutical composition comprising the compound can be used for preparing anti-inflammatory drugs.The application further enriches the structural diversity of active substances of Rhododendron dauricum, which lays a foundation for subsequent related biological activity tests of monomeric compounds, provides active lead compounds for new drug development, and also provides a theoretical basis for in-depth research and development of Rhododendron dauricum medicinal materials.

The invention discloses an odd fruit rhzomorph compound as well as an extraction method and application thereof, belongs to the field of traditional Chinese medicine extraction, and in particular relates to an odd fruit rhzomorph compound which is separated from rhododendron dauricum and is shown in general formulas (I) and (II) and an extraction method of the compound, and also provides the compound or an isomer of the compound, the compound, or a pharmaceutically acceptable salt of the compound or a pharmaceutical composition containing the compound has an inhibition effect on inflammation, and can be used for preparing anti-inflammatory drugs. The structural diversity of active substances of the rhododendron dauricum is further enriched, on the basis, a foundation is laid for carrying out related biological activity tests on subsequently obtained monomeric compounds, an active lead compound is provided for new drug development, and meanwhile, a theoretical basis is provided for deep research and development of rhododendron dauricum medicinal materials. # imgabs0 #

This invention discloses a benzofuran compound and its application in lowering uric acid activity. Compounds 1-3 were isolated from the fermentation products of the endophytic fungus *Septoriella phragmitis*, with compound 1 being a novel compound. The fermentation products were purified using mixed solvent extraction, normal silica gel column chromatography, and high-performance liquid chromatography to obtain compounds 1-3. The inhibitory activity of compounds 1-3 on xanthine oxidase, a target related to gout symptoms, was tested. Experimental results showed that the novel compound 1 exhibited good inhibitory activity against xanthine oxidase. Molecular docking experiments also demonstrated that compound 1 had a good binding energy to the target protein. Therefore, compound 1 can be used to prepare a natural lead compound for delaying or treating diseases caused by xanthine oxidase, providing a potential therapeutic agent for hyperuricemia and gout.

The present invention discloses a series of phenylurea derivative compounds, specifically relating to the compounds as free base, or isomer, or solvate, or pharmaceutically acceptable salt forms; methods of preparing medicaments; compounds composition, and therapeutic uses thereof. The present invention has developed a series of structurally novel compounds based on histamine H3 receptor ligands, and a series of relevant biological tests have been performed on the compounds. The results of the tests all indicate that the compounds have significant H3 receptor antagonistic activity and can be used as lead compounds for the prevention or treatment of H3 receptor-related diseases.

The invention relates to the technical field of chemical synthesis, and particularly discloses an indolone compound and a preparation method thereof. The structure of the indolone compound is shown as a formula (I). The one-step substitution reaction-based indolone compound preparation method provided by the invention has the outstanding advantages of mild reaction conditions, simple operation steps, high product yield and the like, and effectively overcomes the common problems of tedious steps, harsh conditions, poor selectivity and the like in the existing synthesis route. Establishment of an efficient synthesis route provides a reliable way for rapid and large-scale preparation of indolone derivatives with novel structures. The series of novel indolone compounds with potential excellent biological activity provide a new opportunity for discovery of innovative drug lead compounds and development of novel functional materials, and have important research value and wide application prospects. Formula (I)