9 results about "Anti proliferative" patented technology

The invention discloses an antiproliferative synergistic antifungal drug composition based on a notopterygium incisum source, and relates to the technical field of drug preparation, the antiproliferative synergistic antifungal drug composition comprises a first active component and a second active component, the first active component is an anti-proliferative active component and is selected from at least one of the following two compounds: class A: giant column alkane sesquiterpenoids; the class B is a cycloartane type triterpenoid compound; the second active component is a synergistic antifungal active component and is composed of an active component A and an active component B; the pharmaceutical composition takes a specific active component from notopterygium incisum as a core, and can accurately induce apoptosis of target cells, efficiently inhibit proliferation of the target cells, remarkably enhance the antibacterial activity of the antifungal drug and greatly reduce the clinical dosage and toxic risk of the antifungal drug; the natural active components are excellent in biocompatibility and high in medication safety, and can synchronously realize dual effects of disease treatment and infection protection.

The invention discloses a targeted protein degradation agent utilizing a ubiquitin-proteasome pathway as well as a preparation method and application of the targeted protein degradation agent, and belongs to the technical field of biological medicines. On the basis of a PROTAC (protein targeted degradation chimera) strategy and on the basis of imatinib, different Linkers are introduced to be connected with an E3 ubiquitin enzyme ligand Nutlin-3 derivative, a degradation tag is labeled on BCR-ABL cancer protein, and the degradation agent with the Bcr-Abl protein targeting capacity is constructed. A Western blot experiment shows that the targeted protein degradation agent shows a good degradation effect on the Bcr-Abl protein in K562 cells, and the compound WP shows a degradation effect on concentration dependence and time dependence of the Bcr-Abl protein. Tumor cell proliferation experiments show that the compound has certain inhibitory activity on K562 cells. Wherein when the Linker is dodecane-1, 12-diketone, the anti-proliferative activity is the best. An apoptosis experiment and a period experiment show that the targeted protein degradation agent can realize concentration-dependent promotion of cell apoptosis and retard cells in S and G1 / G0 periods.

This invention discloses a KRAS protein degrader modified with norbornene as a hydrophobic group, its preparation method, and its applications. This invention provides a protein degrader with norbornene as the hydrophobic group and MRTX1133 as the KRAS ligand terminus, capable of selectively binding to KRAS (preferably the G12D mutant) and inducing its degradation within cells through a hydrophobic tag, thereby inhibiting downstream oncogenic signaling pathways and suppressing tumor cell proliferation. One objective of this invention is to provide a general synthetic route for this type of degrader and several preferred compound examples (denoted as P1~P7), and to demonstrate methods for detecting its KRAS degradation ability and antiproliferative activity in cell biology experiments (WB, cell viability assays, etc.).

The application discloses a STAT3 / HDAC dual-target inhibitor, a composition and application thereof. A variety of biological experiments prove that the compound has excellent anti-proliferation activity on a variety of cancer cells, has STAT3 and HDAC dual inhibition activity, and has the functions of regulating Ser727 and Tyr705 phosphorylation, and can be used as a STAT3 / HDAC dual-target inhibitor to prepare an anti-tumor and other STAT3 related disease treatment, and has a good application prospect.

The invention belongs to the technical field of medicinal chemistry, and particularly discloses a platinum (IV) prodrug with a small molecule TrxR inhibitor as a ligand and a preparation method and application of the platinum (IV) prodrug, the synthesized platinum (IV) prodrug shows good anti-proliferative activity on cancer cells such as MDA-MB-231, MCF-7, 4T1 and MDA-MB-231 / CDDP, and the anticancer activity of a compound 6b is optimal. In an in-vivo anti-tumor activity test, the compound 6b can effectively inhibit proliferation of cis-platinum sensitive and cis-platinum drug-resistant triple negative breast cancer xenotransplantation tumors, the tumor inhibition rates of the compound 6b are 73.8% and 66.3%, and the curative effect of the compound 6b is superior to that of a positive drug cis-platinum. In addition, the compound 6b can effectively inhibit proliferation of homotransplantation tumors of mouse breast cancer cells 4T1, and the tumor inhibition rate of the compound 6b is 76.8% and is obviously higher than that of a cis-platinum treatment group. And the compound 6b shows a powerful immunoregulation effect in vivo, which indicates that the design successfully realizes effective combination of chemotherapy and immunotherapy, and the compound disclosed by the invention has potential application prospects in treatment of triple negative breast cancer.

The invention provides application of a persimmon leaf flavonoid compound in preparation of a drug for enhancing cis-platinum sensitivity, and belongs to the technical field of biological medicine. The invention provides a nanoparticle formed by self-assembly of a persimmon leaf flavonoid compound and a platinum drug. In-vivo and in-vitro experiment results show that when the persimmon leaf flavonoid compound and the cis-platinum are combined for administration, the killing ability of the cis-platinum to tumor cells can be improved, and when the persimmon leaf flavonoid compound and the cis-platinum are prepared into the nanoparticles (PLF-Cis NPs), the toxicity, the anti-proliferation property and the anti-migration property of the cis-platinum to cancer cells can be greatly further improved. The PLF-Cis NPs can improve the killing effect, promote cell apoptosis and induce cell immunogenic death. According to the invention, the persimmon leaf flavonoid compound is used as the sensitizer for the first time, so that the tumor killing property of platinum drugs can be greatly improved, and a new means is provided for treating tumors or cancers with poor cis-platinum sensitivity.

Disclosed is a cohort of anti-proliferative microRNAs (miRs) wherein each member of the cohort (or combinations thereof) represent a target for modulating cell proliferation (and migration), influencing (or modulating) vascular remodelling and the treatment of various vascular complications, vascular injury vascular disease and (for example) disorders, diseases, syndromes and / or conditions which affect vessels and / or vascular systems of the human or animal body.

This invention discloses a CDK8 / BRD4 dual-target inhibitor, its preparation method, pharmaceutical composition, and applications, relating to the field of medicinal chemistry. The multi-target inhibitory compound designed and synthesized in this invention can effectively inhibit BET and kinase protein activity. The preferred compound has an IC50 value of [missing information]. 50 The concentration can reach nanomolar levels and has excellent anti-proliferative activity against colorectal cancer cells, achieving excellent therapeutic effects at the molecular level, with a very wide range of application prospects; at the same time, the compound preparation method provided by this invention is highly versatile and suitable for various structural types.

The invention discloses a copper (II) complex with anticancer activity as well as a preparation method and application thereof, and belongs to the technical field of complexes. According to the preparation method, CuCl22H2O, CuBr2 or Cu (NO3) 2.3 H2O is subjected to a reaction with benzoyl hydrazone 3-acetyl-7-N, N-diethylamino coumarin respectively, and the complex is obtained. The obtained complex has certain anti-proliferative activity to four cell lines, namely HeLa, MCF-7, A549 and HepG-2, and the anti-proliferative activity is obviously superior to that of a ligand, particularly, the complex shows relatively excellent anti-proliferative activity to the MCF-7 cell line, and the toxicity to normal HUVEC cells is also obviously lower than that of cis-platinum. The copper (II) complex provided by the invention has good anti-cancer activity, the preparation method is simple, the toxicity is small, and a new thought is provided for the development of anti-cancer drugs.