108 results about "Antiproliferative effect" patented technology

The present invention relates to therapeutic combinations and methods of inhibiting the proliferation of cancerous cells, the abnormal growth of cells, and tumor cell growth using the combination of a hedgehog inhibitor with chemotherapy and / or radiation therapy. The present invention also relates to methods of enhancing the antiproliferative effect of chemotherapy and / or radiation therapy in a mammalian cancer patient undergoing either chemotherapy or radiation or a combination of radiation and chemotherapy by co-administering a therapeutically amount of a hedgehog inhibitor, concurrently or sequentially, with the chemotherapy and / or radiation therapy.

An antiproliferative, antiinflammatory, antiinfective, immunization agent of a metal ion chelating agent such as picolinic acid, analogs or derivatives thereof, and methods of using the same. The agents chelate metals in metal containing protein complexes and enzymes required for growth, replication or inflammatory response. The preparations can be administered systemically or topically. The products can be used to reduce systemic levels of metals in disease states such as Wilson's disease, iron or lead toxicity. The preparations have antineoplastic, antiviral, antiinflammatory, analgesic antiangiogenic and antiproliferative effects and are used in the treatment of warts, psoriasis, acne, cancers, sunburn, inflammatory responses, untoward angiogenesis and other diseases and in the prevention of sexually transmitted diseases such as genital warts, herpes and AIDS.

The invention concerns a biocompatible and bioabsorbable wound covering material. The object of the present invention is to improve wound care by a biocompatible, biodegradable wound covering material. In that respect body-specific defense and healing mechanisms are to be assisted and antimicrobial and antiproliferative effects are to be achieved. That is attained in that the wound covering material contains elementary magnesium.

This invention relates to compositions and methods useful for activating LT-β receptor signaling, which in turn elicits potent anti-proliferative effects on tumor cells. More particularly, this invention relates to lymphotoxin heteromeric complexes formed between lymphotoxin-α and multiple subunits of lymphotoxin-β, which induce cytotoxic effects on tumor cells in the presence of lymphotoxin-β receptor activating agents. Also within the scope of this invention are antibodies directed against the lymphotoxin-β receptor which act as lymphotoxin-β receptor activating agents alone or in combination with other lymphotoxin-β receptor activating agents either in the presence or absence of lymphotoxin-α / β complexes. A screening method for selecting such antibodies is provided. This invention also relates to compositions and methods using cross-linked anti-lymphotoxin-β receptor antibodies either alone or in the presence of other lymphotoxin-β receptor activating agents to potentiate tumor cell cytotoxicity.

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.

This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.

The invention relates to a dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis and pruritus. The invention comprises a base anti-inflammatory agent, such as indometacin; one or more optional active ingredients selected alternatively from among at least a corticoid and an antibiotic; and a combination of topical antioxidants used to potentiate the anti-inflammatory effect, selected from among green tea, lipoic acid, curcumin, ascorbyl palmitate, Coenzyme Q10, resveratrol, Pycnogenol™, L-camosine, taurine, vitamin E, vitamin C, papaya extract, isoflavones, manganese, lycopene and quercetin. At least one of the topical antioxidants is a peroxisome proliferator-activated receptor-gamma (PPAR-γ) activator. The invention also includes at least one antioxidant substance with an antiproliferative effect on keratonocytes, e.g. manganese, and at least one substance that blocks tumour necrosis factor-alpha (TNF-α) or other cytokines that provoke the acute phase of the inflammatory reaction, also with an antiproliferative effect, e.g. pentoxifylline.

The invention discloses a compound with an MEK (Mitogen-activated and Extracellular signal-regulated Kinase) inhibiting function as well as a preparation method and application of the compound. The structure of the compound disclosed by the invention is as shown in a formula (I). The preparation method of the compound disclosed by the invention comprises the steps of forming a coumarin ring by adopting a Pechmann reaction mainly and carrying out structural modification of different sites. In the binding experiment of the compound disclosed by the invention and MEK, the binding activity is up to 54.57nM; the anti-proliferation effect IC50 (half maximal inhibitory concentration) value on the melanoma cell A375 is up to 1.23 micrometers; the anti-proliferation effect IC50 value on the colon cancer cell HT-29 is up to 2.13 micrometers; and the activity is higher than that of a positive control U0126. The novel structure type coumarins compound with the MEK inhibiting function shows good MEK binding activity, MEK inhibiting activity, ERK (Extracellular signal Regulated Kinase) pathway inhibiting activity, anti-tumor effect and antiviral effect and has broad application value. The formula (I) is as shown in the specification.

Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.

The invention belongs to the field of medicinal chemistry and particularly relates to 2,4,5-trisubstituted pyrimidine compounds taking FGFRs (fibroblast growth factor receptors) as targets as well as preparation methods and an application of the 2,4,5-trisubstituted pyrimidine compounds. The compounds can selectively inhibit phosphorylation of FGFR kinase so as to be used for treating malignant tumors closely related with the kinase, and can reduce adverse reactions; the compounds can be used for treating tumors related with the FGFR kinase or relevant diseases. The general formula of the 2,4,5-trisubstituted pyrimidine compounds is shown in the specification, wherein R<1>, R<2> and R<3> can be selected from multiple substituents and can be combined randomly. The 2,4,5-trisubstituted pyrimidine compounds taking the FGFRs as the targets have a good inhibition function on the FGFR1 kinase, have an anti-proliferation function on FGFR1-dependent tumor cell line KG1 cells, can be used for preparing antitumor drugs and have better antitumor effects.

A medicament for prophylactic and / or therapeutic treatment of a vascular disease such as vascular restenosis and / or reocclusion after percutaneous transluminal coronary angioplasty using an intravascular stent, which comprises as an active ingredient a substance selected from the group consisting of retinoids and agents for controlling actions of retinoids such as 4-[5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid or a salt thereof, or 4-[[[(3,5-bis-(trimethylsilyl)phenyl]carbonyl]amino]benzoic acid or a salt thereof, wherein said substance has substantially no antiproliferative action on vascular endothelial cells, but substantially has antiproliferative action on vascular smooth muscle cells.

Disclosed are cyanoacrylate polymer particles which comprise an amino acid(s) and have an average particle diameter of less than 1000 nm. The amino acid-containing particles according to the present invention can kill cancer cells by inducing apoptosis-like cell death. The particles have an especially high affinity for cell lines derived from lymphomas such as T-cell lymphoma and B-cell lymphoma. The particles can also exhibit an antiproliferative effect against some kinds of pancreatic cancer-derived cell lines. Therefore, the particles according to the present invention are useful for prevention and / or treatment of cancers.

Cripto, a developmental oncoprotein, antagonizes activin and TGF-b signaling by forming a complex with activin and TGF-b and their type II receptors. This complex precludes the formation of a functional activin / TGF-b•type II•type I complex, thereby blocking the signaling of activin and TGF-b. Cripto may be generally capable of blocking antiproliferative Smad2 / 3 signals and provides a novel mechanism of oncogenic action with multiple therapeutic implications. Inhibiting the formation of Cripto and activin / TGF-b complex may enhance antiproliferative effects of activin and TGF-b.

2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula I that are capable of intracellular chelation of transition metals and of exerting antiproliferative effects in cancer cells, that are cytostatic and / or cytotoxic, are provided. Compounds of Formula I can also induce apoptosis in cancer cells and are thus capable of exerting a cytotoxic effect on cancer cells. The compounds of Formula I are also capable of selectively inhibiting the proliferation of one or more of prostate cancer cells, colon cancer cells, non-small lung cancer cells and leukemia cells. The compounds of Formula I are also capable of increasing the expression of the zinc-regulated tumour suppressor, KLF4 and thus are useful in inhibiting the proliferation of cancer cells in which KLF4 functions as a tumour-suppressor, including, but not limited to, bladder cancer, cancers of the gastrointestinal tract and various leukemias.

The invention relates to a dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis and pruritus. The invention comprises a basic anti-inflammatory agent, such as indometacin; one or more optional active principles selected alternatively from among at least a corticoid and an antibiotic; and a combination of topical antioxidants used to potentiate the anti-inflammatory effect, selected from among green tea, lipoic acid, curcumin, ascorbyl palmitate, Coenzyme Q10, resveratrol, Pycnogenol TM , L-camosine, taurine, vitamin E, vitamin C, papaya extract, isoflavones, manganese, lycopene and quercetin. At least one of the topical antioxidants is a peroxisome proliferator-activated receptor-gamma (PPAR- gamma) activator. The invention also includes at least one antioxidant substance with an antiproliferative effect on keratonocytes, e.g. manganese, and at least one substance that blocks tumour necrosis factor-alpha (TNF- alpha) or other cytokines that provoke the acute phase of the inflammatory reaction, also with an antiproliferative effect, e.g. pentoxifylline.

The invention belongs to the technical field of organic compounds and particularly provides beta-trifluoromethyl vinyl sulfone compounds, a preparation method thereof and an application of the compounds to tumor cell proliferation resistance. The beta-trifluoromethyl vinyl sulfone compounds are prepared from a multicomponent reagent (trifluoromethyl) trimethylsilane (TMSCF3), alkyne, diazonium salt and DABCO.(SO2)2 in an organic solvent DMSO through a one-step reaction. Reaction conditions are quite mild, alkyne bi-functionalization is realized directly through the one-step cascade reaction of the four raw materials, the operation is simple, defects of tedious steps, low operability and yield and poor selectivity of the traditional synthesis method of vinyl sulfone derivatives are overcome, and the method is applicable to large-scale preparation and has quite good application prospect. In-vitro pharmacological activity screening tests show that the compounds have an anti-proliferation effect on tumor cells, part of the compounds have an obvious tumor inhibition activity, the half maximal inhibitory concentration IC50 value can reach mu m level, and the compounds can be used for preparing a kind of novel anti-tumor reagents.

A drug-eluting stent, comprising a base body that is made of an implant material, the base body being partially or entirely covered on the abluminal side with an active ingredient-releasing coating that comprises or is made of a polymer and an active ingredient having an antiproliferative effect, characterized in that the stent's luminal surface and the abluminal surface carrying the active ingredient-releasing coating are covered by a biocorrodible protective layer in a form-fitting manner.

The antiproliferative effects of Icaritin or Desmethylicaritin on cancer cell lines, both in vitro, and in vivo, are disclosed. Experimental data show that Icaritin and Desmethylicaritin dramatically inhibit the growth of most malignant cells. In addition, both Icaritin and Desmethylicaritin have significant Anti-agiogenesis properties, inhibiting or eliminating entirely the development of new malignant cells. Further, no obvious side effects including nausea, hair loss or body weight loss were found in the animals treated with Icaritin or Desmethylicaritin, making both highly effective anti cancer drugs.

A medicament for prophylactic and / or therapeutic treatment of a vascular disease such as vascular restenosis and / or reocclusion after percutaneous transluminal coronary angioplasty using an intravascular stent, which comprises as an active ingredient a substance selected from the group consisting of retinoids and agents for controlling actions of retinoids such as 4-[5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid or a salt thereof, or 4-[[[3,5-bis-(trimethylsilyl)phenyl]carbonyl]amino]benzoic acid or a salt thereof, wherein said substance has substantially no antiproliferative action on vascular endothelial cells, but substantially has antiproliferative action on vascular smooth muscle cells.

Provided herein are compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drug mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof. Moreover, the analogs, like pateamine A, are valuable molecular probes for evaluation of eukaryotic translation initiation and as lead compounds for development of improved anticancer agents.

The invention provides an anti-virus or / and anti-tumor drug and a preparation method thereof and an application of fenugreek biflavone glycosides for preparing anti-virus or / and anti-tumor drugs. The invention provides the application of the chemical component fenugreek biflavone glycosides in fenugreek seeds as drugs for the first time, and uses the fenugreek biflavone glycosides for preparing anti-virus drugs and anti-tumor drugs for the first time. In vivo and in vitro experiment research shows that fenugreek biflavone glycoside tablets or fenugreek biflavone glycoside capsules of the invention have obvious effect on resisting influenza viruses, and the anti-influenza drug effect of the fenugreek biflavone glycoside tablets or fenugreek biflavone glycoside capsules of the invention is superior to the anti-influenza drug effect of the existing Western medicine ribavirin tablets. The anti-HBV effect of the fenugreek biflavone glycoside tablets or fenugreek biflavone glycoside capsules is superior to the anti-HBV effect of kurarinone capsules, and the anti-HIV effect of the fenugreek biflavone glycoside tablets or fenugreek biflavone glycoside capsules is superior to the anti-HIV effect of zidovudine tablets. The fenugreek biflavone glycoside tablets or fenugreek biflavone glycoside capsules have obvious effect on resisting proliferation of liver cancer, gastric cancer, intestinal cancer, lung cancer and cervical cancer cells, and the anti-tumor effect of the fenugreek biflavone glycoside tablets or fenugreek biflavone glycoside capsules is superior to the anti-tumor effect of the existing chemical component preparation hydroxycamptothecine injection.

An antiproliferative effect of IFN-α gene transduction in pancreatic cancer cells. The invention relates to expression of IFN-α to effectively induce growth suppression and cell death in pancreatic cancer cells, an effect which appeared to be more prominent when compared with other types of cancers and normal cells. Another aspect of the invention relates to targeting the characteristic genetic aberration, K-ras point mutation, in pancreatic cancer, and that the expression of antisense K-ras RNA significantly suppresses the growth of pancreatic cancer cells. When these two gene therapy strategies are combined, the expression of antisense K-ras RNA significantly enhanced IFN-α-induced cell death (1.3-3.5 fold), and suppressed subcutaneous growth of pancreatic cancer cells in mice. The invention also relates to a method of suppressing pancreatic cancer cells using double strand RNA formed by antisense and endogeneous K-ras RNA in combination with the anti-tumor activity of IFN-α. The invention relates to the combination of IFN-α and antisense K-ras RNA as an effective gene therapy strategy against pancreatic cancer. The invention also relates to a method of treating pancreatic cancer cells disseminated throughout the body by administering the inventive combination to localized pancreatic cancer cell tumor. The invention also relates to inducing indirect immunological antitumor activity to provide systemic immunity against pancreatic cancer cells.

The invention relates to microRNA-34a and related microRNAs for use in the treatment of B-cell lymphoma. Likewise it relates to microRNA-34a for use in the preparation of a medicament for the treatment of B-cell lymphoma, and for a method of treatment of B-cell lymphoma comprising administering microRNA-34a. These claims are based on the observation that microRNA-34a shows strong anti-proliferative effects when overexpressed in diffuse large B-cell lymphoma (gDLBCL) cell lines, or when delivered intratumorally or systemically in xenograft models of DLBCL.

The invention discloses application of nobiletin, and particularly discloses application of nobiletin in preparation of health products or medicines for preventing and / or treating oral cancer. Through the anti-proliferation effects of monomeric compounds, namely hesperetin, naringenin and nobiletin, in rutaceae citrus fruits and peels on human oral epidermoid carcinoma cells, the experiments show that the hesperetin, naringenin and nobiletin have an obvious effect on inhibiting proliferation of human oral epidermoid carcinoma cells, and the effect of the nobiletin on inhibiting oral cancer cells is most obvious, so that the nobiletin can be used for preparing health products and medicines with effects on preventing and treating oral cancer and is suitable for large-scale popularization and application.

The invention relates to microRNA-34a and related microRNAs for use in the treatment of B-cell lymphoma. Likewise it relates to microRNA-34a for use in the preparation of a medicament for the treatment of B-cell lymphoma, and for a method of treatment of B-cell lymphoma comprising administering microRNA-34a. These claims are based on the observation that microRNA-34a shows strong anti-proliferative effects when overexpressed in diffuse large B-cell lymphoma (gDLBCL) cell lines, or when delivered intratumorally or systemically in xenograft models of DLBCL.

A genus of arylsulfonamide derivatives of aminocycloalkanols is disclosed. The compounds are of the following genus:The compounds induce FOXO1 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 invention discloses application of artesunate and podophyllotoxin conjugates in anti-leukemia drugs according to formula (I) and a preparation method. The preparation method includes using artesunate and podophyllotoxin as raw materials and esterifying to obtain artesunate and podophyllotoxin conjugates according to formula (I). The invention further discloses application of artesunate and podophyllotoxin in anti-leukemia drugs. The conjugates have anti-leukemia cell activity and can be used for preparing anti-leukemia drugs. The artesunate and podophyllotoxin has different degrees of anti-proliferation actions to leukemia K562 cell and leukemia Adriamycin persister K562 / Adr.

Disclosed is an isolated protein from the Chinese medicinal herb, Yuzhu, Polygonatum odoratum (Liliaceae). The protein disclosed is an effective agent showing potent antiviral activities while demonstrating antiproliferative effect on HL-60 leukemia and MCF-7 breast cancer cell lines in vitro. A method of obtaining the target protein and use thereof are also provided.

The invention provides a pyrazolothiazole compound of the formula [I], or a pharmaceutically acceptable salt thereof:The compound of the invention has JAK1 inhibitory activity, and thus, immunosuppressive effect, anti-inflammatory effect and anti-proliferative effect, and is useful in the treatment of the diseases, for example, rheumatoid arthritis, inflammatory bowel disease, psoriasis and vasculitis, bronchial asthma, chronic obstructive pulmonary disease and eosinophilic sinusitis, nasal polyp.