683 results about "Lead compound" patented technology

The invention relates to the field of medicinal chemistry, in particular to a substituted quinolinone compound targeting KRASG12D and application of the substituted quinolinone compound. Pharmacological tests prove that the affinity effect of the synthesized compound on a KRASG12D mutant is superior to that of a lead compound KAL-21404358. The compounds WY1-014 and WY1-062 have ideal inhibition effects on cells of human lung cancer (A549), human melanoma (A375) and human colon cancer (LOVO). The compound WY1-062 has excellent anti-tumor activity, and the activity of the compound WY1-062 is superior to that of cis-platinum.

The invention relates to the field of medicinal chemistry, relates to a general KRAS inhibitor and medical application thereof, and particularly relates to a compound targeting KRAS and mutants KRASG12C and KRASG12D thereof and medical application of the compound. The pharmacological test result of the affinity of KRAS and mutants thereof shows that the affinity of the compound to a KRAS wild type and a KRASG12C mutant type thereof and a KRASG12D mutant type thereof is superior to that of a lead compound, and the compound has a potential inhibition effect on target spots of the KRAS wild type and the KRASG12C mutant type thereof and the KRASG12D mutant type thereof.

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 discloses a five-membered sulfur-containing heterocyclic nucleoside derivative and application thereof in an anti-human immunodeficiency virus (HIV) active medicine, and belongs to the technical field of medicinal chemistry. A series of five-membered sulfur-containing heterocyclic ring nucleoside compounds are synthesized through a Sulfa-Michael / Aldol cascade reaction. The result shows that in an anti-HIV virus test, the five-membered sulfur-containing heterocyclic nucleoside lead compound 42a has the optimal anti-HIV-1 virus activity, and a new structural unit is provided for antiviral candidate drug molecules.

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 relates to an anti-cryptosporidium micromolecular lead compound of a target cryptosporidium helicase. Comprising the following steps: S1, detecting enzyme activity parameters of a drug target helicase (CpeIF4A) and an inhibition effect of Roc-A on the drug target helicase: expressing and purifying a CpeIF4A recombinant protein containing an MBP tag; detecting the enzyme activity; detecting the inhibition effect of the Roc-A on the enzyme activity; determining the affinity between the Roc-A and the CpeIF4A through a heat transfer experiment; s2, in-vitro drug effect determination: evaluating the direct killing capability of Roc-A on sporozoites; the inhibition effect of Roc-A on cryptosporidium is determined through an in-vitro cell infection model, an EC50 value is obtained, and the intracellular period of the Roc-A mainly playing the inhibition effect is determined; detecting the toxicity of Roc-A to host cells to obtain a TC5 value), and obtaining an in-vitro insect-resistant selectivity index (SI); and S3, in-vivo drug effect test: establishing a C57BL / 6IFN-gamma gene knockout mouse infection model to evaluate the effectiveness and safety of Roc-A. The invention determines that the Roc-A has the potential of being further developed into the cryptosporidium-resistant drug, and verifies that the targeted eIF4A can resist cryptosporidium infection.

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 invention discloses a five-membered sulfur-containing heterocyclic nucleoside lead compound and application thereof in anti-hand-foot-and-mouth virus active drugs, and belongs to the technical field of medicinal chemistry. A series of five-membered sulfur-containing heterocyclic ring nucleoside compounds are synthesized through a Sulfa-Michael / Aldol cascade reaction. A result shows that in an anti-EV-A71 virus test, the five-membered sulfur-containing heterocyclic ring nucleoside lead compounds 33a, 5b and 30b have relatively good anti-EV-A71 virus activity, and a new structural unit is provided for antiviral candidate drug molecules.

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 invention discloses a preparation method and application of a novel glycoside component in eupatorium chinense. The 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, HW-40F gel column chromatography, high performance liquid chromatography and other methods to obtain a new glycoside compound. The inhibitory activity of the separated compound on diabetes related targets alpha-glucosidase and protein tyrosine phosphatase 1B (PTP1B) is tested, the experimental result shows that the compound has good inhibitory activity on two enzymes, and the molecular docking experiment also shows that the compound has good inhibitory activity on the two enzymes. The compound has good binding energy with two target protein alpha-glucosidase and protein tyrosine phosphatase 1B. Therefore, the compound can be used for preparing medicines for preventing, delaying or treating alpha-glucosidase or PTP1B-mediated diseases, especially type II diabetes and obesity, or can be used as a lead compound of the medicines.

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 phenanthro [9, 10-d] imidazole quaternary ammonium salt derivative as well as preparation and antibacterial application thereof. According to the series of compounds, phenanthro [9, 10-d] imidazole quaternary ammonium salt derivatives which are novel in structure and good in antibacterial activity are prepared by taking phenanthro quinone as a lead compound and modifying the structure of phenanthro quinone, the structural general formula of the phenanthro [9, 10-d] imidazole quaternary ammonium salt derivatives is shown in the specification, and R is selected from H, C6-C14 alkyl or C3-C8 alkylene. The phenanthro [9, 10-d] imidazole quaternary ammonium salt derivative prepared by the invention has a relatively good antibacterial effect on gram-positive bacteria such as staphylococcus aureus S.aureus ATCC 29213 and various clinical methicillin-resistant staphylococcus aureus (MRSA), meanwhile, the water solubility is improved, the biotoxicity of a parent body is reduced, and the phenanthro [9, 10-d] imidazole quaternary ammonium salt derivative has relatively high yield and is suitable for industrial production. The compound is expected to be further developed into a clinical candidate antibacterial drug. # imgabs0 #

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 provides application of B-AP15 in preparation of antituberculosis drugs, and particularly belongs to the technical field of drug preparation. The B-AP15 is used for preparing the antituberculous drugs and has relatively good inhibitory activity on MTB standard strains, MTB sensitive strains and clinical drug-resistant strains, so that a drug lead compound and a drug candidate are provided for development of the novel antituberculous drugs, and the B-AP15 has important significance on prevention and / or treatment of tuberculosis.

The invention discloses an application of a sulfanyl acetamide compound with a structure shown in a formula I in preparation of a medicine for preventing and / or treating tumors and idiopathic pulmonary fibrosis. The compound can be stably combined with key amino acid residues of DDR1 protein, has a remarkable inhibition effect on phosphorylation activation of the DDR1 protein and various tumor cells, plays an anti-tumor role by effectively inhibiting protein activity, and provides an effective lead compound for subsequent drug design. # imgabs0 #

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 provides a synthesis method of a novel inhalable liposome and an application of the novel inhalable liposome in ARDS (arterial thrombosis syndrome) treatment, and the synthesis method comprises the following steps: firstly, mixing DSPE-PEG2K-TK-NHS and tocilizumab (TCZ: Tocilizumab) to form a lead compound DSPE-PEG2K-TK-TCZ; the preparation method comprises the following steps: dissolving DPPC, cholesterol, DSPE-TK-PEG2k and FG4592 in 5mL of chloroform, carrying out reduced pressure evaporation in a sample bottle to form a film, and adding 3mL of deionized water to prepare Lip-coated RF; and then stirring and incubating the DSPE-PEG2K-TK-TCZ and the Lip (at) RF, so as to form the Lip (at) RFT. As a functional nano-material with ultra-small size, good biocompatibility, excellent ROS removal capability and ROS responsive drug release, the nano-material is used for treating ARDS. The invention has the advantages that: the Lip-coated RFT relieves lung oxidative stress, inflammatory response, protein permeability and histological severity in the LPS-induced mouse ALI model. Therefore, Lip at RFT can be used as a new way for treating ARDS. Aerosol inhalation of Lip-coated RFT can effectively improve the severity of ARDS.

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 directed evolution strategy of type II sesquiterpene cyclase (SsDMS) derived from Streptomyces shedoensis based on alanine scanning, and an application of the type II sesquiterpene cyclase (SsDMS) derived from Streptomyces shedoensis based on alanine scanning. The invention relates to a plurality of SsDMS key mutant sites capable of catalytically generating a novel drive type sesquiterpenoid compound, which comprise substitution of sites 208, 248, 249, 497 and 505, and the SsDMS key mutant sites comprise substitution of sites 208, 248, 249, 497 and 505. The invention discloses an efficient escherichia coli cell factory applied to heterologous expression of an SsDMS mutant and efficient production of a novel drive type sesquiterpene compound, and further obtains the drive type sesquiterpene compound with a novel structure. According to the present invention, the efficient production of the drive type sesquiterpene compound by using the SsDMS and the mutant thereof is achieved, the modification strategy has wide applicability, the important enzymology resource is provided for the biosynthesis of the novel terpene compound, and the more choices are provided for the discovery of the drug lead compound.

The invention discloses a diosgenin derivative containing a 1, 2, 3-triazole structure fragment as well as a preparation method and application of the diosgenin derivative, and belongs to the field of natural medicinal chemistry and medicinal chemistry. Based on a molecular heterozygosis principle, diosgenin is used as a lead compound and is heterozygous with a 1, 2, 3-triazole structure fragment with different substituent groups to obtain a derivative shown as a general formula (I) or (I). The diosgenin derivative containing the 1, 2, 3-triazole fragment, disclosed by the invention, has good anti-breast cancer activity. Pharmacological experiment results show that the anti-tumor activity of part of the derivatives on human breast cancer cells is obviously superior to that of diosgenin, and the toxicity on human normal gastric mucosa epithelial cells is relatively small, so that the derivatives are expected to be further developed into anti-tumor drugs. # imgabs0 #

The invention belongs to the field of lead compound library construction in medical research, and particularly relates to a construction method of an On-DNA aryl sulfide structure compound, which comprises the step of reacting On-DNA aryl mercaptan or On-DNA aryl thiophenol with a halide to generate the On-DNA aryl sulfide structure compound, the step is a photocatalytic reaction at room temperature, and the on-DNA aryl sulfide structure compound is obtained. The wavelength of the light source for reaction is 315-455 nanometers, the solvent for reaction comprises an organic solvent and water, and the organic solvent in the solvent is one or more of dimethyl sulfoxide, N, N-dimethylformamide and dimethylacetamide. The oligomeric nucleic acid-aryl sulfide structure compound with rich structures can be obtained at a time under the reaction conditions, the reaction conditions are wide in adaptability and obviously superior to the prior art, the oligomeric nucleic acid-aryl sulfide structure compound is suitable for being used as a reaction raw material of a first-stage or second-stage halide, and the conversion rate of a third-stage iodide can also reach 90% or above.

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.