40 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 relates to the field of medicinal chemistry, in particular to a substituted benzenesulfonamide compound and application thereof. Pharmacological experiment results show that the benzenesulfonamide compounds have strong inhibitory activity on GSTP1-1 protein, and part of the compounds have anti-proliferation effects on tumor cells of human lung cancer, cis-platinum drug-resistant lung cancer and the like, and have a certain degree of cis-platinum drug resistance reversing capability.

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 present invention discloses a kind of spiro[benzofuran-tetrahydropyrrole] compounds, a preparation method and an application thereof. In the present invention, benzofuran aza-diene and β-sulfonamido-substituted enoate are used as reaction raw materials, and under the action of an organophosphorus catalyst, spiro[benzofuran-tetrahydropyrrole] compounds are efficiently obtained through a one-step reaction. The present invention has the following advantages: the organophosphorus catalyst is cheap and easily available, stable in air and has no pungent odor; there is no need to add transition metals as catalysts, oxidants or reductants, strong acids or strong bases; the present invention has a wide application range, is economical and practical, and is environmentally friendly; the reaction substrates are easy to prepare; the reaction is easy to scale up and has practical value. In addition, such compounds have a significant anti-proliferation effect on the tested human gastric cancer cells (HGC-27) and human liver cancer cells (HepG2), and have certain anti-cancer activities.

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 compound capable of being used as a BET / p300 bromodomain double-target inhibitor or a derivative thereof as well as a preparation method and application of the compound. The compound has a structure as shown in a formula I, wherein substituent groups R1 to R4 in the formula # imgabs0 are defined in the specification. The invention also relates to a pharmaceutical composition containing the compound or the derivative thereof, application of the compound or the derivative thereof as a BET / p300 bromodomain double-target inhibitor, and a preparation method of the compound or the derivative thereof. The compound or the derivative thereof can significantly inhibit the activity of BET / p300 bromodomain, has a significant anti-proliferation effect on cancer cells and multiple myeloma cells, and also has good metabolic stability, safety and drug-likeness, so that the compound or the derivative thereof has a wide application prospect.

The invention discloses a functional small molecule peptide based on eggshell membrane peptide and application of the functional small molecule peptide in drug delivery, and belongs to the field of biological medicine. The invention relates to a functional small molecule peptide based on eggshell membrane peptide, which has pH responsiveness, can target liver cancer, can be prepared into a drug-loaded self-assembly body, and has a structural formula shown in Figure 1. The invention designs a novel small molecule peptide, develops a novel combined treatment scheme of a COX-2 inhibitor and a chemotherapeutic drug, and combines the anti-proliferation effect of DOX and the pro-apoptosis effect of CXB, so as to improve the therapeutic effect of the CXB. The activity of COX2 and the activation of hepatic stellate cells are inhibited, and the synergistic effect of resisting liver cancer is realized. Especially, the pH responsiveness of the experimental peptide Pep is utilized, morphology transformation occurs in a subacid environment, drug excretion and liver cancer proliferation are inhibited, and the functional small molecule peptide capable of enhancing the effect and reducing the toxicity provides a new treatment choice for liver cancer patients.

The invention relates to the technical field of biological medicine, in particular to a synthesis method and application of pinenyl thiazolidone derivatives, and the synthesis method comprises the step of synthesizing thiosemicarbazide A at the yield of 90% under the promotion of hydrochloric acid through condensation reaction between myrtenal and 4-methyl-3-thiosemicarbazide. Cyclizing the compound A and chloroacetic acid to obtain a key intermediate thiazolidone B; then, the intermediate reacts with substituted benzaldehyde, and the target compound C1-C13 is obtained. The adopted substrate myrtenal has a better anti-proliferation effect on malignant cells, strong water solubility is enhanced by introducing thiazolidines, and remarkably enhanced anti-cancer activity can be shown by introducing the thiazolidine derivative modified by Schiff base. The series of products are novel in structure, high in yield, simple in separation and purification operation and suitable for mass production, and part of products such as C5 have good biological activity.

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 present invention provides a PROTAC compound derived from triptolide, a preparation method and an application, relating to the technical field of PROTAC compounds. The structure of the PROTAC compound derived from triptolide is shown in Formula I; in Formula I, X is -(CH2) m - or -CH2CH2(OCH2CH2) n -, m is any integer from 2 to 8, and n is any integer from 1 to 3. Through activity tests, the PROTAC compound derived from triptolide has significant anti-proliferation effects on various cancer cells such as colorectal cancer, lung cancer, breast cancer, etc., and its toxicity has decreased significantly. It is expected to prepare new anti-cancer drugs and has good development prospects. #imgabs0#

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.

Compounds which are thiazole and triazole 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 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 present inventors have discovered that in living organisms that have received an antigen-binding molecule containing an antigen-binding domain whose binding activity to an antigen changes depending on ion concentration conditions and containing an FcRn-binding domain having FcRn-binding activity in a neutral pH range, immune responses to the antigen are induced. Furthermore, the present inventors have discovered that in living organisms that have received an antigen-binding molecule containing an antigen-binding domain whose binding activity to an antigen changes depending on ion concentration conditions and containing an FcRn-binding domain having FcRn-binding activity in a neutral pH range, immune responses to the antigen are induced, and also the antigen-binding molecule has cytotoxicity or antiproliferative action against cancer cells, foreign biological species, or such that express the antigen to which the antigen-binding molecule binds.

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.