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168 results about "Beta-Carboline" patented technology

Β-Carboline (9H-pyrido[3,4-b]indole), also known as norharmane, is a nitrogen containing heterocycle. It is also the prototype of a class of compounds known as β-carbolines.

1-substituted 1,2,3,4-tetrahydro-beta-carboline and 3,4-dihydro-beta-carboline and analogs as antitumor agents

A composition includes a substituted dihydro- or tetrahydro-beta-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-beta-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.
Owner:NATIONAL YANG MING UNIVERSITY +1

Beta-carboline pharmaceutical compositions

A soft capsule containing a solution or suspension of a PDE5 inhibitor, and use of the capsule in treating sexual dysfunction.
Owner:ICOS CORP

Banisterine derivative compound and uses thereof

The present invention relates to a harmine derivative compound and the application. The compound is produced through the structural modification of the 1st, 2nd, 3rd, 7th and 9th pint of the parent nuclear of the beta-carboline of the harmine; thus the novel harmine derivative compound is synthesized with the enhanced anti-tumor activity and no toxicity of the nervous system. Through the screening research of the vitro and vivo anti-tumor model, the harmine derivative compound is found to have the significant anti-tumor activity (the tumor-inhibition rate of the tumor-bearing mice model reaches as high as 63.5 percent), have no neurotoxicity, and have the prospects of clinical application. The preparation method of the compound is simple; the collection rate is high; and the compound is used for the drugs of treating various tumor diseases.
Owner:XINJIANG HUASHIDAN PHARMA RES

1-Aryl or 1- Heteroaryl-Pyrido(B)indoles and Uses Thereof

Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure:where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.
Owner:BUOLAMWINI JOHN K

Beta-carboline alkali derivative compounds and application thereof

The invention relates to beta-carboline alkali derivative compounds and application thereof. Novel beta-carboline alkali derivative compounds are synthesized by structurally modifying the first, third and ninth sites of beta-carboline parent nucleus and importantly introducing amido into the first and third sites; and the obvious anti-tumor activity of the compounds is kept, and the water solubility of the compounds is improved. A method for preparing the compounds is simple and convenient, the yield is high, and the beta-carboline alkali derivative compounds can be used for preparing medicines for treating various tumor diseases.
Owner:新疆华世丹药业股份有限公司

Hybridized peptide with 3S-tetrahydrochysene-beta-carboline-3-carboxylic acid as connecting arm, preparation method and application thereof

InactiveCN101318993AExcellent thrombolytic activityPeptide/protein ingredientsPeptidesThrombusCarboxylic acid
The invention discloses a general formula I compound and a general formula II compound having thrombus dissolving activity, a preparation method thereof and an application thereof as thrombus dissolving agent. The invention adopts a rat carotid-jugular vein bypass intubation thrombus model to evaluate the thrombus dissolving activity of the general formula I compound and the general formula II compound respectively. Animal experimental results show that: both the general formula I compound and the general formula II compound have excellent thrombus dissolving activity and can be applied to clinical practice as a thrombus dissolving agent.
Owner:PEKING UNIV

HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use

Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.
Owner:AGOURON PHARMA INC

Novel indoletriazole alkaloid as well as preparation method and antifungal application thereof

The invention relates to the technical field of medicines and discloses an indoletriazole alkaloid antifungal compound with a novel framework, i.e. fructus evodiae triazole alkali (3-[2-N-methyianiline]-triazolo[4,3-a]-3,4-dihydto-beta-carboline) which is a compound with a brand-new framework. The invention also relates to a preparation method and application of the indoletriazole alkaloid antifungal in the field of medicines. Particularly, the compound has strong antifungal activity, and compared with the antifungal medicaments clinically applied at present, the compound has the advantages of high efficiency, low toxicity, broad antifungal spectrum, and the like, opens a new approach for deeply researching and developing new antifungal medicaments and can be used for preparing new antifungal medicaments.
Owner:INST OF BOTANY JIANGSU PROVINCE & CHINESE ACADEMY OF SCI

RGD tetrapeptide modified beta-carboline acyl-tryptophan and preparation, nanostructure, activity and application thereof

The invention discloses RGD tetrapeptide modified beta-carboline acyl-tryptophan and discloses a preparation method, a nanostructure, an effect of resisting tumor cell adhesion, an effect of resisting tumor cell invasion, an effect of resisting tumor cell migration, an anti-rumor effect and an effect of inhibiting tumor transfer to lung. The invention discloses application thereof in medicine. The formula is as shown in the specification.
Owner:CAPITAL UNIVERSITY OF MEDICAL SCIENCES

Beta-carboline alkaloid and application thereof to preparing antimalarial medicaments

The invention discloses a beta-carboline alkaloid and application thereof to preparing antimalarial medicaments. The structure of the beta-carboline alkaloid is as shown in a formula (I) described in the specification. The beta-carboline alkaloid disclosed by the invention or pharmaceutical salt thereof plays a killing role on plasmodia, can be used for preparing the antimalarial medicaments and treating plasmodium infectious diseases and provides more drug choices for treating malaria. R is expressed in the formula (I), wherein R1=OMe, OH or H.
Owner:SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI

Heterocyclic carboxylic acid-modified thymopentins and their preparation method, anti-tumor effect and use

The invention discloses heterocyclic carboxylic acid-modified thymopentins. The heterocyclic carboxylic acid-modified thymopentins have a general formula I. In the general formula I, RCO represents 1,2,3,4-tetrahydro-beta-carboline-3-formyl, beta-carboline-3-formyl, 1,2,3,4-tetrahydroisoquinol-3-formyl, isoquinol-3-formyl, 1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-formyl, 1-methyl-beta-carboline-3-formyl or 4,5,6,7-tetrahydro-3H-imidazo[4,5-C]pyridyl-6-formyl. The invention also discloses a preparation method of the heterocyclic carboxylic acid-modified thymopentins, and in-vitro tumor cell proliferation-resistant activity of the heterocyclic carboxylic acid-modified thymopentins. The invention further discloses heterocyclic carboxylic acid-modified thymopentin activity of inhibiting weight gain of a tumor in a S180 tumor-loading mice, and use of the heterocyclic carboxylic acid-modified thymopentins in preparation of anti-tumor drugs. The general formula I is RCO-Arg-Lys-Asp-Val-Tyr.
Owner:CAPITAL UNIVERSITY OF MEDICAL SCIENCES

Trp-Trp-Trp pentapeptide modified beta-carboline, preparation therefor, nanostructure, activity and application thereof

The invention discloses 1-(4-isopropyl propyl)-beta-carboline-3-formyl-Trp-Trp-Trp-Lys-Glu structured as follows, a preparation method therefor, a nanostructure thereof, antitumor action thereof, action thereof in resisting adhesion and invasion and migration of tumor cells, and illustrates application thereof in medical science. The formula is shown in the description.
Owner:CAPITAL UNIVERSITY OF MEDICAL SCIENCES

Beta-carboline modified by KE as well as preparation, nanostructure, activity and application of the same

The invention provides beta-carboline modified by KE as well as preparation, nanostructure, activity and application of the same. The invention discloses 1-(4-hydroxy-3-methoxycarbonyl phenyl)-[beta]-carboline-3-formyl-Lys-Glu having a following structure shown in the description, wherein the standard abbreviation of Lys-Glu is KE, and discloses a preparation method thereof, a nanostructure thereof, an anti-tumor effect thereof, and effects on resisting tumour cells adhering to invade and migrating thereof. Further, the invention discloses anti-inflammatory effect of the same, and explains the application in medical science.
Owner:CAPITAL UNIVERSITY OF MEDICAL SCIENCES

3-Position diamine beta-carboline alkali compound, and preparation method, medicinal composition and use thereof

The invention discloses a 3-position diamine connected beta-carboline alkali compound, and a preparation method, a medicinal composition and a use thereof. The above di-beta-carboline alkali compound and its medicinal salt are represented by general formula I, and the preparation method of the di-beta-carboline alkali compound comprises the following steps: carrying out a condensation reaction on two molecules of beta-carboline-3-formaldehyde and one molecule of diamine NH2(CH2)nNH2, and hydrogenating. The invention also discloses the medicinal composition, and an application of the di-beta-carboline alkali compound in the preparation of antitumor medicines. The medicinal composition comprises an effective amount of the di-beta-carboline alkali compound represented by the formula I and a pharmacodynamically acceptable carrier. The antitumor medicines are used for treating melanoma, stomach cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermal cancer, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer and colon cancer.
Owner:XINJIANG HUASHIDAN PHARMA RES

Green synthetic method of beta-carboline compound

InactiveCN103864787AHigh yieldEasy to prepare and safe and environmentally friendlyOrganic chemistryPictet–Spengler reactionCarboxylic acid
The invention discloses a green synthetic method of a beta-carboline compound. The green synthetic method of the beta-carboline compound is technically characterized by comprising the following steps: carrying out Pictet-Spengler reaction on L-tryptophan to prepare tetrahydro-beta-carboline-3-carboxylic acid; and decarboxylating and oxidizing the tetrahydro-beta-carboline-3-carboxylic acid under the effect of an oxidizing decarboxylating agent hydrogen peroxide to prepare the beta-carboline compound. The invention discloses specific synthetic steps and main reaction equations in the preparation process. The method disclosed by the invention has the advantages of simple preparation and safety and environmental-friendliness, and the yield of the beta-carboline compound is high, so that the demand on green chemistry is satisfied.
Owner:HENAN NORMAL UNIV

Copper chloride complex using 1-(2-pyridine)-9-hexyl-beta-carboline as ligand and synthesis method and application thereof

The invention discloses a copper chloride complex using 1-(2-pyridine)-9-hexyl-beta-carboline as a ligand and a synthesis method and application thereof. A structural formula of the complex is shown as the following formula (I). The synthesis method comprises the steps that the compound shown as a following formula (II) and copper chloride are taken and dissolved in a polar solvent to perform complexing reaction, wherein the polar solvent is selected from one or more of methyl alcohol and ethyl alcohol and one or more of water, acetone, chloroform, dichloromethane and N,N-dimethylformamide. The complex shows the stronger antitumor activity than the ligand and cis-platinum, has a good potential medicinal value and is hopeful for preparation of various antitumor drugs. The structures shown by the formulas (I) and (II) are shown in the description.
Owner:GUANGXI NORMAL UNIV

Method for detecting picrasma quassioides alkali content in picrasma quassioides

The invention relates to the analytical chemistry field, particularly to a method for detecting picrasma quassioides alkali content in picrasma quassioides. The method comprises the following steps: preparing 1-carbomethoxy-Beta-carboline, nigakinone, and metiiylnigakinone standard solutions and drawing a standard curve; drying and smashing picrasma quassioides, and extracting to obtain a solution to be detected; detecting, wherein the detection chromatographic condition is that a C18 chromatographic column is adopted, the column temperature is 20-40 DEG C, the detection wave length is 205-280 nm, acetonitrile is taken as an A phase of a mobile phase while acid water is taken as a B phase of the mobile phase, the flow velocity is 1 mL / minute, and the elution procedures are performed in the way that the volume percent of acetonitrile is changed from 5% to 45% during the period from 0 minutes to 35 minutes, from 45% to 80 % during the period from 35 minutes to 40 minutes, from 80% to 90% during the period from 40 minutes to 50 minutes, and from 90% to 95% during the period from 50 minutes to 60 minutes; computing the content of three kinds of picrasma quassioides alkali as per the standard curve, wherein acids in acid water are phosphoric acid, formic acid or acetic acid, and the volume fraction of acid in acid water is 0.1-1%. The method can be used for the ration of three kinds of picrasma quassioides alkali at one time.
Owner:GUANGZHOU BAIYUSN HUTCHISON WHAMPOA CHINESE MEDICINE

Carboxylic acid derivatization beta-carboline and preparation method thereof

The invention relates to carboxylic acid derivatization beta-carboline and a preparation method of the carboxylic acid derivatization beta-carboline. The method comprises the steps that organic solvent is added into the mixture of 6-methyl-beta carbazoline, metal-salt catalyst and initiator, oxygen is introduced, and after stirring reaction is conducted, the reaction is terminated; filtering is conducted, and solid crude products are collected; further purification of the crude products is conducted through recrystallization and silica gel column chromatography to obtain products. According tothe method, reaction conditions are mild, the application range of substrates is wide, and a large number of beta-carboline derivatives with diversified structures can be obtained.
Owner:NINGBO UNIV

Beta-carboline compound and synthetic method and application thereof

The invention relates to a beta-carboline compound and a synthetic method and application thereof, and belongs to the technical field of medicine. The structure of the compound is shown as the formula I (the formula I is shown in the specification). After an initial test, it is indicated that the in-vitro anti-renal-fibrosis activity of the compound is remarkable, the treatment effect on renal interstitial fibrosis caused by obstruction of the left ureter of a Balb / c mouse is good, the good potential medical value is achieved, and the beta-carboline compound and the synthetic method and application thereof can be used for preparing various kinds of anti-renal-fibrosis and anti-chronic-kidney-disease medicine.
Owner:GUANGXI NORMAL UNIV
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