17 results about "Antiproliferative effect" patented technology

2-diarylmethyl-4-aminotetrahydropyran derivatives are disclosed. The compounds include the following genus:or a pharmaceutically acceptable salt thereof. The compounds activate cellular PP2A, suppress oncogenic kinase signaling and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

Novel kisspeptin-13 or KP-13 peptides and KP-13 satellites or modified peptides (KPSATs) are disclosed having improved therapeutic benefits in regulating pathophysiological changes in various tissues, particularly lung tissue. These KPSATs have improved antiproliferative effects and non-cytotoxic effects on airway smooth muscle cells and tissue.

2-diarylmethyl-4-aminotetrahydropyran derivatives are disclosed. The compounds include the following genus:or a pharmaceutically acceptable salt thereof.The compounds activate cellular PP2A, suppress oncogenic kinase signaling and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

The application provides a benzene [d] isoxazole compound and an application thereof. The compound has the structure shown in the following formula I. The benzene [d] isoxazole compound provided by the application can induce degradation of BET protein and / or GSPT1 protein, and has an anti-proliferation effect on cancer cells. Therefore, the compound and the composition provided by the application can be used for preparing a drug for treating or preventing tumor formation, inflammation, viral infection, cell proliferative disorder, autoimmune disease, sepsis and the like.

The invention relates to a pharmaceutical composition of an extract of Agarophyton chilensis, with antiproliferative effect in prostate cancer, comprising(a) 0.1 to 90% of an oleoresin of Agarophyton chilensis, with the following major components: palmitic acid, arachidonic acid, oleic acid, stearic acid, meristic acid, linoleic acid; and(b) 10 to 99.9% excipients and formulation aids for different pharmaceutical forms.And its use to prepare a drug for the treatment or prevention of prostate cancer and other hyperproliferative states of prostate tissue cells.

The invention discloses a polysubstituted amine compound, a pharmaceutical composition containing the polysubstituted amine compound and an application of the polysubstituted amine compound in tumor resistance. The structure of the polysubstituted amine compound is shown as a formula I in the specification. Through multiple experiments, the inventor of the invention proves that the compound disclosed by the invention has a remarkable inhibiting effect on FBXO44, and can be combined with the FBXO44 in cells to inhibit down-regulation of the FBXO44 on MTSS1, so that the formation of tumor cell microfilament skeletons is disturbed, and the compound has a strong anti-proliferation effect on gastric cancer cell strains such as NUGC4 and the like. Therefore, the compound disclosed by the invention can be used as an FBXO44 inhibitor to be applied to medicines for treating solid tumors or leukemia related to human or animal cell proliferation.

The present disclosure relates to a pyrido[3,4- d]pyrimidin-8-one derivative compound exhibiting excellent anti-proliferative effects against cancer cells, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, a production method therefor, a pharmaceutical composition for preventing, alleviating or treating cancer metastasis and proliferative disease containing the same as an active ingredient, and an anti- cancer composition against cancer cells. The compound exhibits excellent cancer cell inhibitory activity and anti- proliferative effects, and thus is effective in inhibiting cancer cells, preventing cancer metastasis and proliferative diseases or treating cancer. The compound is selected from a pyrido[3,4-d]pyrimidin-8-one derivative compound represented by the following formula, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a stereoisomer thereof: [Image disponible dans le document PDF, Image available in the PDF document]

The present application relates to a kind of arylamide compounds or its pharmaceutically acceptable salt or its stereoisomer with the structure shown in formula I, formula II, formula III or formula IV, and its application.The arylamide compound provided by the present application is a molecular glue degrader for Bcr-Abl T315I , which can effectively degrade wild-type Bcr-Abl kinase and mutant Bcr-Abl T315I Kinase, can effectively inhibit the kinase activity of Bcr-Abl and Bcr-Abl T315I Mutant, has good anti-proliferation effect on tumor cells carrying Bcr-Abl and Bcr-Abl T315I ;And selectivity is good, side effect is small, and safety is good.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a phenyl-pyrazole-benzene ring propylamine derivative and application thereof. The phenyl-pyrazole-benzene ring propylamine derivative disclosed by the invention is a compound shown as a formula (I) or a pharmaceutically acceptable salt thereof. The compound provided by the invention simultaneously contains characteristic groups such as substituted phenyl, pyrazole, cyclopropylamine and the like. Tests prove that the phenyl-pyrazole-benzene ring propylamine derivative disclosed by the invention has a nanomole-level inhibition effect on LSD1 at an enzyme level, shows remarkable biological inhibition activity on the LSD1, and can be used for preparing drugs for targeted inhibition of the LSD1. The compound is further subjected to anti-cancer activity research on acute myelogenous leukemia, and the compound is found to have a relatively strong anti-proliferation effect on acute myelogenous leukemia cells, so that the compound has a relatively good treatment effect on acute myelogenous leukemia, and can be developed as a lead medicine for resisting acute myelogenous leukemia.

The non-small cell lung cancer adenocarcinoma via the pathway mediated with the cannabinoid receptor is targeted for the first time with the synthetic cannabinoid agonist arachidonoyl cyclopropylamide (ACPA). An ACPA-PCL nanoparticle release system based on nanoengineering provides long term-controlled release and stability of the CB1 receptor agonist ACPA following the determination of the efficient dose and the antiproliferative effect of ACPA on the non-small cell lung cancer lines expressing the cannabinoid (CB) receptors in vitro medium at different doses.

The application discloses a dihydroindole compound and a synthesis method and application thereof, and relates to a dihydroindole compound obtained by taking o-aminobenzaldehyde and allyl carbonate as reaction raw materials and under the mediation of an organic phosphine reagent. Advantages of the application include: high reaction efficiency, high yield, cheap, stable, and non-irritating smell of the organic phosphine reagent, no need to add an oxidizing or reducing agent, relatively mild conditions, no need to use a transition metal as a catalyst in the reaction, economy and practicability, environmental friendliness, easy preparation of a reaction substrate, high reaction efficiency after reaction amplification, and practical value. The compound has significant anti-proliferation effect on all tested human pancreatic cancer cells (PANC-1) in a growth period, and has certain anticancer activity.

The present invention relates to two drug molecules having the structure of Formula I and Formula II, which have an antiproliferative effect against cancer, and to the synthesis of these molecules.

The present disclosure relates to a pyrido[3,4-d]pyrimidin-8-one derivative compound exhibiting excellent anti-proliferative effects against cancer cells, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, a production method therefor, a pharmaceutical composition for preventing, alleviating or treating cancer metastasis and proliferative disease containing the same as an active ingredient, and an anti-cancer composition against cancer cells. The compound exhibits excellent cancer cell inhibitory activity and anti-proliferative effects, and thus is effective in inhibiting cancer cells, preventing cancer metastasis and proliferative diseases or treating cancer.

Deubiquitinase-targeting chimeras (DUBTACs) are an emerging class of therapeutics that can stabilize tumor suppressors by hijacking a deubiquitinase (DUB), thereby offering a strategic pivot from conventional approaches to target tumor suppressors. However, only OTUB1 and USP7 have been harnessed for DUBTAC development to date. Here, we show for the first time that USP28 can be leveraged for developing DUBTACs. Utilizing a USP28 non-covalent ligand, we crafted USP28-recruiting DUBTACs that effectively stabilized the ΔF508-CFTR mutant protein, with comparable effectiveness to the previously reported OTUB1- and USP7-recruiting CFTR DUBTACs. Furthermore, we developed USP28-recruiting cGAS DUBTACs that effectively stabilized cGAS, elevated the cGAS-STING signaling pathway, and elicited an anti-proliferative effect. We also developed first-in-class PPARγ DUBTACs to intervene with cancer metabolism pathways. Our lead PPARγ DUBTACs effectively stabilized PPARγ and suppressed the proliferation in cancer cells, thus providing a new potential anti-cancer therapeutic approach. Hence, this work advances the targeted protein stabilization field.

The application provides a glycyrrhizin metal complex, a preparation method thereof and application thereof in preparation of anti-tumor and anti-inflammatory drugs, and belongs to the technical field of anti-tumor drugs. The glycyrrhizin is metal-complexed with cobalt, nickel and rubidium to construct a hexokinase inhibitor. The results of examples show that, compared with the NS group, the glycyrrhizin metal complex provided by the application exhibits a significant inhibitory effect on hexokinase, and has a good anti-proliferation effect on A549 (human non-small cell lung cancer cells), MCF-7 (human breast cancer cells), SK-Mel-28 (human malignant melanoma cells) and SW480 (human pancreatic cancer cells). In addition, the glycyrrhizin metal complex provided by the application improves the inhibitory activity of glycyrrhizin on OH free radicals, and has stronger anti-inflammatory activity than glycyrrhizin.

The invention provides a beta-carboline compound as well as a preparation method and anti-tumor and antibacterial application thereof. The related beta-carboline derivative has the advantages of novel structure, high anti-proliferative activity, high CDK4 / 6 inhibitory activity and high pseudomonas aeruginosa activity. The synthesized compounds ZFXH-1 to ZFXH-29 have a relatively high anti-proliferation effect on two colorectal cancer cells, the MIC values of most of the compounds ZFXH-1 to ZFXH-29 are greater than or equal to 256 mu g / mL, and the yield of pyocyanin can be remarkably reduced under high concentration. The invention also finds that the ZFXH-3 and clinically common antibiotics have a synergistic antibacterial effect on a standard strain PAO1 and a clinical strain XN-1. Therefore, the beta-carboboline derivative provided by the invention plays an important role in preparing medicines for treating tumors and resisting the activity of pseudomonas aeruginosa.

The present disclosure relates to a 7-amino-3,4-dihydropyrimidopyrimidin-2-one derivative compound exhibiting excellent anti-proliferative effects against cancer cells, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, a production method therefor, a pharmaceutical composition for preventing, alleviating or treating cancer metastasis and proliferative disease containing the same as an active ingredient, and an anti-cancer composition against cancer cells. The compound exhibits excellent cancer cell inhibitory activity and anti-proliferative effects, and thus is effective in inhibiting cancer cells, preventing cancer metastasis and proliferative diseases or treating cancer.