31 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.

The invention belongs to the technical field of drug synthesis, and particularly relates to a novel nitrogen heterocyclic compound, the structure of the novel nitrogen heterocyclic compound is shown as a formula (I), and the novel nitrogen heterocyclic compound has an anti-proliferation effect on multiple tumor cell lines, and can be applied to anti-tumor drugs, especially acute myelogenous leukemia drugs.

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.

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 present invention improves an effect of killing or an effect of inhibiting the growth of cancer cells. The present invention comprises: a binding domain that includes a first antigen-binding site that binds to a cancer cell and a second antigen-binding site that binds to a T cell; a cleavable sequence that is linked to the binding domain; and a masking moiety that is linked to the N-terminus of a single-chain antibody via the cleavable sequence when the binding domain is composed of the single-chain antibody, and that is linked to the C-terminus of each light chain via the cleavable sequence when the binding domain is composed of heavy chains and light chains. In a state in which the cleavable sequence is cleaved, the masking moiety functions as an agonist of a co-stimulatory molecule for the T cell or an antagonist of a co-inhibitory molecule for the T cell.

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 invention discloses a (9β-H)-pimarane skeleton diterpenoids with anti-colon cancer activity and a derivative thereof, and further discloses a preparation method and application of the compounds above; the invention finds that novel skeleton compounds 1 and 2 have certain inhibition effects on colon cancer cells, wherein the compound 2 has remarkable anti-proliferation effects on two colon cancer cell lines HT-29 and SW620, and the effects are both stronger than those of a positive drug 5-fluorouracil, so that the compound has the potential of being developed into a new anti-colon cancer drug.

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]

3-Diarylmethylenes are disclosed. The compounds activate 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.

3-Diarylmethylenes are disclosed. The compounds activate 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 present invention relates to the field of medicinal chemistry, specifically to a class of substituted benzenesulfonamide compounds and their applications. Pharmacological experiments have shown that the benzenesulfonamide compounds of the present invention have strong inhibitory activity against GSTP1-1 protein. Some compounds have anti-proliferative effects on tumor cells, including human lung cancer and cisplatin-resistant lung cancer, and have a certain degree of ability to reverse cisplatin resistance.

Compounds which are oxadiazaborole derivatives are disclosed, including compounds of the following genus:The compounds are inhibitors of hematopoietic cell kinase (HCK) and exhibit anti-fibrotic and anti-proliferative effects. They are useful in the treatment of a variety of disorders, including a fibrosis or a fibrotic disease, such as renal fibrosis.

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 invention relates to an aryl amide compound with a structure as shown in a formula I, a formula II, a formula III or a formula IV, or pharmaceutically acceptable salt or stereoisomer thereof, and application thereof. The aryl amide compound provided by the invention is a molecular glue degradation agent aiming at Bcr-AblT315I, can effectively degrade wild type Bcr-Abl kinase and mutant type Bcr-AblT315I kinase, can effectively inhibit the kinase activity of Bcr-Abl and Bcr-AblT315I mutants, and has a relatively good anti-proliferation effect on tumor cells carrying Bcr-Abl and Bcr-AblT315I; the selectivity is good, toxic and side effects are small, and the safety is good.

The present invention discloses a dihydropyrazole-azepine compound, a pharmaceutical composition containing the same, and its use in anti-tumor treatment. The structure of the dihydropyrazole-azepine compound is shown in Formula I. The inventors of the present invention have confirmed through multiple experiments that the compound of the present invention has a significant inhibitory effect on AKT1, exhibiting a potent anti-proliferative effect on tumor cell lines such as mouse neuroblastoma Neuro2a cells and a potent differentiation-inducing effect on Neuro2a cell lines. Therefore, the compound of the present invention can be used as a differentiation-inducing regulator and / or AKT inhibitor in drugs for treating solid tumors or blood cancers associated with cell proliferation and differentiation abnormalities in humans or animals.

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.

The present invention discloses a rosin acid derivative, a preparation method, and an application thereof. The rosin acid derivative has significant anti-proliferative activity against glioma cells, can achieve a significant anti-glioma proliferation effect at relatively low concentrations, and has good tumor treatment effects. The compound with outstanding activity has low hepatotoxicity and exerts an anti-proliferative effect on glioma cells in a time- and concentration-dependent manner. In addition, the representative rosin acid derivative has a pKa value within the range of 6.2 to 7.2, has good blood-brain barrier permeability, and is conducive to entering the brain to exert its medicinal effect.

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 application discloses a marine fungus-derived steroidal compound, a preparation method thereof and application of the steroidal compound in preparation of an antitumor drug. A structural formula of the steroidal compound is shown as formula (I). The compound has a strong antiproliferation effect on MDA-MB-435S, HepG2, SKOV3, SKOV3R, A2780, A549 and various tumor cells, and can be used for preparing an antitumor drug, especially an anti-melanoma, liver cancer, ovarian cancer and lung cancer drug, thereby providing a new drug for treatment of various tumors. In addition, the compound is derived from a natural microorganism and can be obtained through microbial fermentation, and the preparation method is simple. Therefore, the steroidal compound has good clinical application potential in antitumor treatment and has important application value.

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.

The invention relates to an application of CNP0221572 and / or CNP0053696 as an IDH1 / 2 inhibitor, and belongs to the technical field of biological medicines. According to the present invention, the research results show that the compound CNP0221572 and the compound CNP0053696 have excellent inhibition effects on the activity of mutant enzymes IDH1 R132H and IDH2 R140Q, and have anti-proliferation effects on IDH1 R132H mutated human brain glioma cells (U87MG cells) and IDH2 R140Q mutated human blood leukemia cells (TF-1 cells), and the compound CNP0221572 and the compound CNP0053696 have good anti-proliferation effects on the human brain glioma cells (U87MG cells) and the IDH2 R140Q mutated human blood leukemia cells (TF-1 cells), the compound can be used as an IDH1 / 2 inhibitor (IDH1 / 2 mutant double-target inhibitor). According to the invention, a new choice is provided for the IDH1 / 2 inhibitor, and a drug selection library for diseases related to mutation of IDH1 and IDH2 is enriched.