44 results about "Antileukemic agent" patented technology

The present invention relates to a new use of the compound chlorogenic acid isolated from the piper betel leaf extract or from any other sources for the treatment of acute and chronic myeloid leukemia and lymphoid leukemia, and the present invention also provides a pharmaceutical composition comprising chloregenic acid along with pharmaceutically acceptable additive for the treatment of acute and chronic myeloid leukemia and lymphoid leukemia.

The invention discloses efficient targeting drug-loaded nano-micelle as well as a preparation method and application thereof. The preparation method comprises the following steps: (1) dissolving an amphiphilic block copolymer into an organic solvent, and then adding small molecule anti-leukemia drug hydrochloride; after the materials are fully dissolved and evenly mixed, adding triethylamine to remove hydrochloric acid so as to form a small molecule anti-leukemia drug; then, adding the small molecule anti-leukemia drug into a phosphate buffer solution (PBS) to form nano-micelle which has a hydrophilic shell and a core encapsulated with the drug; carrying out dialysis, and drying to obtain the drug-loaded nano-micelle; a polydopamine modification method is used for modifying a specific antibody against a leukemia cell surface antigen, thus realizing targeting. The drug-loaded nano-micelle prepared by the method has a particle size of 50-100nm, is very good in monodispersity, has a higher drug loading capacity and encapsulation efficiency, is simple in targeted modification step and good in targeted killing effect of leukemia cells, but is high in biosecurity for normal cells, and can realize slow release so as to avoid the defects caused by long-term and multiple dosing.

The invention belongs to the field of preparation of drugs, and discloses application of flavonoid GL-V9 in preparation of anti-leukemia drugs. The flavonoid GL-V9 can guide acute myeloid leukaemia cells to become into dendritic cells, and can be used for preparing anti-leukemia drugs.

The invention relates to an acute myeloid leukemia miRNA and transcription factor model and a construction method and application thereof. The construction method includes: acquiring differential expression miRNA and different expression transcription factors of marrow samples of acute myeloid leukemia patients and a healthy contrast group, constructing a miRNA-transcription factor regulatory network model to obtain core miRNA and core transcription factors, and the like. The constructed miRNA and transcription factor model can be used for construction of diagnosis probes, chips or reagents, equipment and the like to provide intermediate result information or reference information for diagnosis of the acute myeloid leukemia patients. By the acute myeloid leukemia miRNA and transcription factor model, microRNA mediated network regulation contents are enriched, and an action mechanism of a microRNA and transcription factor mediated regulation network in AML (acute myeloid leukemia) is revealed. Research results lay the foundation for development of anti-leukemia medicines or biological products, and high application value is achieved.

The invention discloses aloe-emodin quaternary ammonium salt alkyl iodoacetates with the multiple-related anti-cancer mechanism and a preparation method thereof. The preparation method comprises the steps that firstly, aloe-emodin reacts with phosphorus tribromide to obtain brominated aloe-emodin; secondly, brominated aloe-emodin reacts with N-methyldi-n-octylamine to generate aloe-emodin quaternary ammonium salt; lastly, the aloe-emodin quaternary ammonium salt reacts with chloroacetyl chloride to generate iodine acetylation in the presence of sodium iodide to obtain aloe-emodin quaternary ammonium salt alkyl iodoacetates shown as a structural formula (please see the structural formula in the description). In-vitro cancer cell inhibition tests of aloe-emodin quaternary ammonium salt alkyl iodoacetates show that aloe-emodin quaternary ammonium salt alkyl iodoacetates has the good inhibitory activity on hematopoietic cells, is expected to be developed into anti-leukemia drugs and has the great application prospect.

The invention discloses an application of Vandetanib to preparation of a targeted EphB4 anti-tumor drug, and belongs to the technical field of medicines. Experiments verify the application of the Vandetanib, and a molecular docking method, an SPR (surface plasmon resonance) method and MST (modulated scatterer technique) experiment results indicate that the Vandetanib can interact with EphB4. EphB4kinase experiments display that the Vandetanib can obviously inhibit EphB4 kinase activity. Proliferation of leukemic cells K562, JLTRG and H9 is remarkably inhibited. Besides, the Vandetanib remarkably inhibits expression of signal molecules p-PI3K p85/p55 and PI3K p85 at the downstream of the EphB4, and the phosphorylation level of MEK (methyl ethyl ketone) and ERK (extracellular signal-regulated kinase) is reduced. Therefore, the experiment results sufficiently support the application of the Vandetanib to an anti-leukemia drug and the targeted EphB4 anti-tumor drug.

The invention discloses an indoledione piperazine type alkaloid and a preparing method and application thereof. The alkaloid is obtained from fermentation products of a garcinia multiflora endophyticfungus through separation and purification, wherein the endophytic fungus has the name of Aspergillus sp.GZWMJZ-258, is preserved in the China Center for Type Culture Collection on April 28th, 2019 atthe address of Wuhan, China, and has the preservation number of CCTCC NO:M 2019305. The indoledione piperazine type alkaloid is a compound with a new framework. It is shown through a pharmacologicalexperiment that the alkaloid has a certain selective retraining effect on a leukemia cell line MV4-11 and can be applied in an anti-leukemia medicine.

The invention provides pyrrolo[2,3-b]pyrazine derivatives. The structural formula of the derivatives are disclosed as Formula (I), wherein R1 is hydrogen, hydroxyl, heterocyclic radical, phenyl or substituted phenyl, and amido or substituted amido; R2 is cyano, methyl or hydrogen; n=1, 2, 3, 4, 5, 6, 7 or 8; Y is NH, O, S or N(CH2)mR5; m=1, 2, 3, 4, 5 or 6; and R5 is hydrogen, amido or substituted amido. The derivatives provided by the invention can obviously inhibit activity of DNA topoismerase II and inhibit high expression of the DNA topoismerase II in tumor cell strains, and is an important target for antineoplastic drugs. Meanwhile, the derivatives have obvious inhibiting actions on proliferation of multiple tumor cell strains, have obvious capacity for inducing apoptosis of leukaemia cells, and have wide application prospects in preparing antitumor and anti-leukaemia drugs.

The invention relates to succinyl hydrazine compounds derivative and medical compound containing them; and the application of it in preparing medicine that resists leukemia. The succinyl hydrazine compounds derivative shows inhibiting action to BCR-Ab1 tyrosine kinase activity through pharmacological test. It is characterized by high effecivity and low toxicity, and can be widly used to prepare medicine that treats chronic granulocytic leukemia (CML) and philadelphia chromosome positive acute lymphoblastic leukemia, especially medicine treating patient that generates drug resistance to Gleevec.

The present invention provides the compound Ormeloxifene [3,4-trans-2,2-dimethyl-3-phenyl-4-p-(beta-pyrrolidinoethoxy)phenyl-7-methoxy chroman] as useful in inducing differentiation in wide range of myeloid leukemias including acute promyelocytic leukemia, acute myeloid leukemia and chronic myeloid leukemia where block in differentiation is common feature. Ormeloxifene induced differentiation that is marked by increase in differentiation marker proteins like C/EBPα and surface proteins such as cd11b and granulocyte colony stimulating factor receptor (GCSFr). Differentiated cells having neutrophil like morphology were observed when treated with 1.0 uM to 7.5 uM ORM which clearly indicates that ORM can induce differentiation in myeloid leukemia cells. At higher doses (5 uM to 7.5 uM) there is early onset of myeloid differentiation (24 to 48 h) with reduced no. of cells which is likely due to apoptotic effects of ORM at higher does. In contrary, lower doses (1 uM) induce differentiation after longer duration (6-15 days) with quite reduced apoptotic effect.

The invention relates to the field of drug synthesis and biological activity evaluation, in particular to an aminomethylpyridine derivative, a preparation method and application thereof. The aminomethylpyridine derivative adopts aminomethylpyridine and substituted benzaldehyde as the raw materials, and the obtained aminomethylpyridine derivative has a general structural formula shown as the specification. The aminomethylpyridine derivative provided by the invention has mild synthesis conditions, and simple and easily operable post-treatment method, thus being suitable for industrial production. Compared with the existing anti-leukemia drug imatinib, the aminomethylpyridine derivative has significant inhibitory effect on human chronic granulocytic leukemia cell line K562, and is suitable for further screening as an anti-leukemia drug.

The invention discloses new application of mercaptopurine and derivatives thereof, namely application of mercaptopurine and derivatives thereof in preparation of drugs for removing malignant tumor immunosuppression, mercaptopurine and thioguanine act on tumor cells of human lung cancer, colorectal cancer, liver cancer, melanoma, breast cancer and the like. The expression of glycosyltransferase GLT8D1 can be remarkably reduced. Further, the protein level and glycosylation level of PDL1 are inhibited, so that the killing effect of peripheral blood mononuclear cells on tumor cells is improved, and the purpose of inhibiting tumors is achieved; the invention finds that mercaptopurine/thioguanine which interferes with nucleic acid biosynthesis and is widely applied to anti-leukemia drugs can inhibit glycosyltransferase GLT8D1 and a programmed cell death ligand 1 (PDL1) in a targeting manner to enhance tumor killing of T cells so as to achieve the purpose of drugs for treating various tumors; The invention provides a new therapeutic drug for treating various tumors.