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385 results about "HeLa" patented technology

HeLa (/ˈheɪlɑː/; also Hela or hela) is an immortal cell line used in scientific research. It is the oldest and most commonly used human cell line. The line was derived from cervical cancer cells taken on February 8, 1951 from Henrietta Lacks, a patient who died of cancer on October 4, 1951. The cell line was found to be remarkably durable and prolific, which warrants its extensive use in scientific research.

Dimer compound of guaiane type sesquiterpenes and uric acid as well as extraction and separation method and application of dimer compound

The invention relates to the field of natural products, in particular to a dimer compound of guaiane type sesquiterpenes and uric acid as well as an extraction and separation method and application of the dimer compound. According to the invention, a new dimer compound of guaiane type sesquiterpene and uric acid is extracted and separated from carpesium abrotanoides in Guizhou, and it is found that the dimer compound has relatively strong anti-tumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharynx cancer, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an optional scheme for broad-spectrum anti-cancer drugs. Moreover, in human prostate cancer cells PC3, human cervical cancer cells Hela, human liver cancer cells HepG2 and human glioma cells U87 which are resistant to paclitaxel, the compound also shows strong anti-cancer activity, which indicates that the compound has the potential of treating patients resistant to paclitaxel.
Owner:KUNMING MEDICAL UNIVERSITY +1

Kit for detecting antibody of myasthenia gravis and preparation method of kit

The invention relates to a kit for detecting a myasthenia gravis antibody and a preparation method of the kit. The kit for detecting the myasthenia gravis antibody comprises the following components: a myasthenia gravis antibody detection plate, a working solution, PBS (Phosphate Buffer Solution), a fluorescent secondary antibody and a mounting medium, wherein the myasthenia gravis antibody detection plate is prepared by mixing hela cells containing MUSK, LRP4, Titin and RYR1 proteins with modified polystyrene and then spotting the mixture on a glass slide; the modified polystyrene is obtained by reacting chloromethyl polystyrene resin with dopamine. According to the present invention, the existence of the four antibodies such as MUSK, LRP4, Titin and RYR1 can be simultaneously detected in the same system. The multiple detection mode can comprehensively reflect the antibody spectrum of the myasthenia gravis patient, reduce the sample size and the detection time, reduce the detection cost, and improve the detection efficiency and the clinical application value.
Owner:BEIJING JINGYI MEDICAL TESTING LAB CO LTD

VEGFR2-HDAC6 dual inhibitor containing chalcone fragment as well as preparation method and application of VEGFR2-HDAC6 dual inhibitor

The invention provides a VEGFR2-HDAC6 dual inhibitor containing chalcone fragments as well as a preparation method and application of the VEGFR2-HDAC6 dual inhibitor, and relates to the technical field of medicinal chemistry. The invention discloses a VEGFR2-HDAC6 dual inhibitor containing chalcone fragments. The structural formula of the VEGFR2-HDAC6 dual inhibitor is shown as a formula A, according to the invention, the VEGFR2-HDAC6 dual inhibitor containing the chalcone fragment and having a novel structure is designed and synthesized by utilizing a splicing principle, the anti-proliferative activity test is carried out on cervical cancer cells Siha and chronic granulocytic leukemia cells K562, and the result shows that the VEGFR2-HDAC6 dual inhibitor containing the chalcone fragment provided by the invention has relatively good inhibitory activity on the Siha cells and the K562 cells.
Owner:BOZHOU UNIV

Copper complex with anticancer activity and preparation method and application thereof

The invention belongs to the field of anti-cancer metal complexes, and particularly relates to a copper complex with anti-cancer activity and a preparation method and application thereof. Cu (OAc) 2H2O and coumarin-3-formyl-(2-aminomethylpyridine) are respectively dissolved in a solvent, the two solutions are mixed and stirred at room temperature to react for a period of time, the reaction solution is filtered, the filtrate is sealed and naturally volatilized at room temperature for 3-7 days, the complex can be obtained, the IC50 value of the complex to Hela cervical cancer cells is 0.8964 + / -0.09 mu M, and the IC50 value of the complex to Hela cervical cancer cells is 0.8964 + / -0.09 mu M. According to the present invention, the inhibition effect of the complex on HeLa cervical cancer cells is 3.38 times of the inhibition effect of cis-platinum, the toxicity of the complex on normal cells but HUVEC is very small, IC50 is greater than 100 [mu] M, and the complex has a high selectivity coefficient SI (SI = normal cell IC50 / cancer cell IC50), and the selectivity coefficient SI is greater than 111 and is 584 times of the selectivity coefficient of cis-platinum (SI = 0.19). The complex has the capability of inducing apoptosis of cancer cells and has concentration dependence. Meanwhile, the complex can retard cancer cells and an S phase so as to inhibit cell proliferation, and can generate an intercalation effect with HS-DNA (High-Speed Deoxyribose Nucleic Acid).
Owner:NANJING FORESTRY UNIV

Synthesis and antitumor activity research of novel drug micromolecule containing phenothiazine structure

The invention discloses synthesis and antitumor activity research of a novel drug small molecular formula (1) containing a phenothiazine structure. R is # imgabs 1 #. 10H phenothiazine is used as an initial raw material, (E)-3-(10-ethyl-10H-phenothiazin-3-yl) acrylic acid is generated through a typical Friedel-Crafts alkylation reaction, an NBS bromination reaction and the like, and then an important intermediate compound 6 is synthesized through a Wittig reaction and a hydrolysis reaction. And carrying out coupling reaction on the intermediate compound 7 and different amine compounds to obtain 11 target compounds 7a-7k: formula (1). A CCK-8 experiment is carried out on a target compound to obtain a conclusion that the target compound 7a-7k and 5-fluorouracil are tested at the concentration of 20 mu M, and the result shows that the compound 7f has the best inhibition effect on A549, Hep G2 and HeLa cells, and the compound 7c has the better inhibition effect on the A549 cells. IC50 value calculation is carried out on a target compound under various concentrations, the IC50 value of 7c to HELA cells is small, the IC50 value of 7f to Hep G2 and HeLa cells is minimum, and the inhibition effect is the best. Therefore, the compound can be used for antitumor drugs.
Owner:CHANGCHUN UNIV OF TECH

Aromatic polyketone compound as well as preparation method and application thereof

The invention relates to the technical field of biological medicine, and discloses an aromatic polyketone compound as well as a preparation method and application thereof. According to the aromatic polyketone compound, a compound I and a compound II are separated from an ethyl acetate extract of rice fermentation liquor of Crystalomyces hyricus, and the compound I and the compound II are respectively named as Crystaloketide A and Crystalomycin D. In-vitro anti-cancer activity tests are carried out on the Crystaloketide A and the Crystalomycin D. According to the aromatic polyketone compound disclosed by the invention, the anti-cancer activity of the Crystaloketide A and the Crystalomycin D. Results show that the compound I and the compound II have the effects of inhibiting human cervical cancer cells, human liver cancer cells, human nerve cancer cells and human pancreatic cancer cells respectively, so that the compound I and the compound II can be further prompted to be used for preparing anti-cancer drugs.
Owner:KUNMING UNIVERSITY

Paeonol Mannich base-rhein conjugate as well as preparation method and application thereof

The invention belongs to the technical field of medicinal chemistry, and discloses a paeonol mannich base-rhein conjugate as well as a preparation method and application thereof. The conjugate is a compound as shown in a general formula (I) or (II) or a pharmaceutically acceptable salt thereof. Compared with the clinically common antitumor drugs fluorouracil and paeonol, the conjugate provided by the invention has obviously higher in-vitro anti-human hepatoma carcinoma cell (HepG2) and human lung cancer cell (A549) proliferative activity, and the in-vitro anti-human cervical carcinoma cell (Hela), human colon cancer cell (HT29) and human osteosarcoma cell (U2OS) proliferative activity of most compounds is obviously superior to that of fluorouracil and paeonol; and the conjugate has good water solubility, is expected to be applied to treatment of various cancers such as cervical cancer, colon cancer, osteosarcoma, lung cancer or liver cancer, and has a wide clinical application prospect. # imgabs0 #
Owner:ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE

Secondary metabolite of fennel endophytic fungus fusarium oxysporum as well as preparation method and application of secondary metabolite

The invention belongs to the field of plant endophytic fungus secondary metabolites, particularly relates to a secondary metabolite of fennel endophytic fungus fusarium oxysporum as well as a preparation method and application thereof, and provides a fennel endophytic fungus secondary metabolite with structures as shown in compounds 1-8. Wherein the compound 2 and the compound 7 have inhibitory activity on staphylococcus aureus, escherichia coli, bacillus cereus, bacillus subtilis, candida albicans and shigella, and have a certain inhibitory effect on cervical cancer Hela cell strains.
Owner:KUNMING UNIV OF SCI & TECH

3-sulfamoyl benzamide compound as well as preparation method and application thereof

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 3-sulfamoyl benzamide compound as well as a preparation method and application thereof. The 3-sulfamoyl benzamide compound has a structure as shown in a formula I. In the formula I, X is chlorine or trifluoromethyl; r1 and R2 are independently C1-4 alkyl or R1, R2 and N atoms connected with R1 and R2 jointly form a heterocyclic group, and the heterocyclic group is a substituted or unsubstituted five-membered or six-membered heterocyclic group; and when the heterocyclic group is a substituted heterocyclic group, the substituent group in the substituted heterocyclic group is one or more of C1-4 alkyl, phenyl and acetyl. The 3-sulfamoyl benzamide compound disclosed by the invention has a remarkable proliferation inhibition effect on HCT116 colon cancer cells, HeLa human cervical cancer cells, MDA-MB-231 human breast cancer cells and A375 human malignant melanoma cells.
Owner:PEKING UNIV

Single cell viability assessment method based on cell nucleus geometric parameters and Bayesian deep learning fusion model and application of single cell viability assessment method

PendingCN121073941AImage analysisNeural learning methodsPattern recognitionBiochemical markers
The invention discloses a single cell activity evaluation method based on cell nucleus geometric parameters and a Bayesian framework, which comprises the following steps: establishing a HeLa cell activity gradient model through adriamycin induction, carrying out cell nucleus segmentation by adopting Cell pose 3.0 and extracting 26 geometric features, screening a high-confidence sample in combination with a Bayesian deep learning framework, and evaluating the activity of a single cell according to the high-confidence sample. And constructing a multi-modal feature fusion model to integrate geometric features and deep semantic features, and finally realizing unmarked and high-precision single cell activity evaluation. The method overcomes the limitation that a traditional technology depends on biochemical markers, has the advantages of being easy and convenient to operate, high in flux and high in interpretability, and provides an innovative technical means for tumor liquid biopsy and precise medical treatment.
Owner:NINGBO UNIV

Preparation and purification method and application of quinoline derivative with biological activity

The invention discloses a preparation and purification method and application of a quinoline derivative with biological activity, and belongs to the technical field of medicine synthesis. According to the key points of the technical scheme, the quinoline derivative molecule has a structure # imgabs0 #, wherein X is NH or empty (benzene rings are directly connected); r is an aromatic ring derivative or alkyl or other groups. The invention designs and synthesizes a quinoline derivative with a novel structure, and the compound has a relieving effect on LPS-induced microglial cell inflammation and has a certain inhibition effect on cervical cancer cells.
Owner:HENAN UNIV OF SCI & TECH

Bionic MOF nano platform capable of dual-targeting cervical cancer tumor cells and cancer-related fibroblasts and co-delivering FAK inhibitor and bismuth as well as preparation method and application of bionic MOF nano platform

The invention provides a bionic MOF nano platform capable of double targeting cervical cancer tumor cells and cancer-related fibroblasts and co-delivering an FAK inhibitor and bismuth as well as a preparation method and application thereof, the bionic MOF nano platform comprises an MOF material loaded with the FAK inhibitor (IN10018) and bismuth (Bi), and a hybrid membrane coating the outer part of the MOF material loaded with the FAK inhibitor and the bismuth, the hybrid membrane is obtained by mixing and physically extruding a cervical cancer tumor cell (HeLa and SiHa) membrane and a cancer-related fibroblast (CAFs) membrane. According to the bionic MOF nano platform, in an acid environment, the ZIF-8 nano particles loaded with the IN10018 and the Bi disintegrate, the IN10018 is released, CAFs infiltration in tumors is reduced, meanwhile, due to addition of the Bi, the radiation absorption efficiency is improved, and the sensitivity of the tumors to radiotherapy is further enhanced through a double-targeting mechanism.
Owner:WUHAN LVDONG MEDICAL TECH CO LTD

Ruthenium complex as well as preparation method and application thereof

The invention discloses a ruthenium complex as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis. The polypyridine ligand and the ruthenium dimer are combined through the substitution reaction, the chelate of the polypyridine ligand and the ruthenium aromatic hydrocarbon is obtained, the synthesis process is simple, the cost is low, and the chelate can be combined with an existing medicine to improve and enhance the medication curative effect. The prepared ruthenium complex can effectively inhibit cancer cell proliferation, and especially shows an excellent anti-proliferation effect on cervical cancer cells. And the liposome can improve the lipophilicity / lipophilicity of the ruthenium medicines and increase the stability of the medicines, and has better anti-tumor activity compared with platinum medicines and unmodified ruthenium medicines.
Owner:CHONGQING MATERNAL & CHILD HEALTH HOSPITAL (CHONGQING OBSTETRICS & GYNECOLOGY HOSPITAL CHONGQING INST OF GENETICS & REPRODUCTION)

Monoclonal antibody for detecting E6 protein in cervical cancer cell nucleus and application thereof

The invention provides a monoclonal antibody for detecting E6 protein in cervical cancer cell nucleus and application of the monoclonal antibody. The invention provides the monoclonal antibody which is high in specificity, strong in affinity, stable in expression, good in repeatability and capable of specifically recognizing the HPV 16E6 protein in a cell nucleus, especially the HPV 16E6 protein, and has the potential of being used for preparing medicines for preventing and treating cervical cancer.
Owner:ATTOGEN BIOMEDICAL SUZHOU INC

A biomimetic MOF nanoplatform capable of dual-targeting cervical cancer tumor cells and cancer-associated fibroblasts and co-delivering FAK inhibitors and bismuth, as well as its preparation method and application

The present invention provides a biomimetic MOF nanoplatform that can dual-target cervical cancer tumor cells and cancer-associated fibroblasts and co-deliver FAK inhibitors and bismuth, and its preparation method and application. The biomimetic MOF nanoplatform includes a MOF material loaded with FAK inhibitors (IN10018) and bismuth (Bi), and a hybrid membrane coated on the outside of the MOF material loaded with FAK inhibitors and bismuth. The hybrid membrane is obtained by physical extrusion after mixing cervical cancer tumor cell (HeLa and SiHa) membranes and cancer-associated fibroblast (CAFs) membranes. In an acidic environment, the biomimetic MOF nanoplatform of the present invention disintegrates ZIF-8 nanoparticles loaded with IN10018 and Bi, releases IN10018, reduces CAFs infiltration in the tumor, and at the same time, the addition of Bi improves radiation absorption efficiency, further enhancing the sensitivity of the tumor to radiotherapy through a dual-targeting mechanism.
Owner:XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV

Probe set, kit and nucleic acid signal amplification in-situ hybridization detection method

The invention discloses a probe set, a kit and a nucleic acid signal amplification in-situ hybridization detection method, and relates to the technical field of molecular biology, the probe set comprises: a labeled extension probe, the sequence of which is as shown in SEQ ID No.9-24; and the sequence of the closed probe is as shown in SEQ ID No. 25-27. The kit comprises the probe set, a signal amplification precursor, a signal amplification body and an alkaline phosphatase labeled probe. According to the present invention, the partial probe sequence introduces the non-natural bases, and can be used for detecting the HPV18 infected cervical cancer Hela cells, the experiment results show that the introduction of the non-natural bases does not affect the normal positive value, the matching degree between the non-natural bases is more specific than the matching of the natural bases, and the detection sensitivity is improved.
Owner:CHENGDU NUO SEN MEDICAL LAB CO LTD

Construction method and application of Uusu figure virus report replicon

The invention discloses a construction method and application of a Uusu figure virus report replicon. According to the invention, a low-copy plasmid pACYC-177B is used as a carrier, all non-structural proteins and non-coding region genes of USUV are retained, 38 amino acids before the N terminal of C protein are retained in the structural protein part, 45 amino acids behind the C terminal of E protein are retained in the structural protein part, and a NanoLuc luciferase tag is inserted between the retained C and E protein genes to obtain a pACYC-TMN-Nlucc-Rep report replicon. The Uu figure virus report replicon pACYC-TMN-Nluc-Rep constructed in the invention can normally work on cells such as BHK21, Vero, DF-1, Hela and the like, and can be effectively translated and replicated. Therefore, the USUV report replicon pACYC-TMN-Nlucc-Rep constructed in the invention can be used as an important research tool to be applied to the research of the USUV.
Owner:SICHUAN AGRI UNIV

Preparation method and application of electrochemical biosensor for dynamically monitoring Cyt c in tumor cells based on rapid scanning voltammetry

The invention discloses a preparation method and application of an electrochemical biosensor for dynamically monitoring Cyt c in tumor cells based on fast scanning voltammetry. The preparation method is characterized by comprising the following steps: 1) preparing a PtNE nano electrode; (2) preparing the PtNE / Apt nano electrochemical biosensor; and (3) accurately puncturing the PtNE / Apt electrode into cytoplasm of a single Hela cell through a three-dimensional micro-control system, so that Apt and intracellular Cyt c are specifically combined and subjected to conformational change, and 3 '-end modified Fc is close to the surface of the electrode, thereby generating a remarkable electrochemical signal. The change of Fc redox peak current is dynamically monitored through fast scanning voltammetry, the quantitative relation between the Cyt c concentration and the peak current is established, and the relation between the Cyt c concentration and the cell activity is monitored according to the quantitative relation. The device has the advantages of high sensitivity, excellent anti-interference capability and remarkable signal amplification effect.
Owner:NINGBO UNIV

5, 9-di-tert-butyl naphtho-indolizino phenothiazine compound as well as preparation method and application thereof

The invention relates to a 5, 9-di-tert-butyl naphtho-indolizine phenothiazine compound as well as a preparation method and medical application thereof. The compound is efficiently synthesized through Ullmann coupling and palladium-catalyzed intramolecular arylation reaction. In-vitro anti-tumor activity research shows that the compound has remarkable selective inhibitory activity on various human tumor cell lines, and particularly, the inhibitory effect on non-small cell lung cancer A549 cells (IC50 = 0.21 mu M) is improved by two orders of magnitude compared with that of cis-platinum; iC50 (half maximal inhibitory concentration) of other cell lines are as follows: 1.26 mu M of prostate cancer PC-3 cells, 6.78 mu M of liver cancer HepG2 cells, 7.99 mu M of cervical cancer Hela cells and 25.46 mu M of breast cancer MCF-7 cells. Preliminary toxicity experiments prove that the compound has the characteristic of low cytotoxicity. The compound can be used as a novel high-efficiency low-toxicity anti-tumor lead compound, and provides an important structural basis for the development of anti-cancer drugs.
Owner:NANJING FORESTRY UNIV

Transfection reagent based on blank lipid nanoparticles as well as preparation method and application of transfection reagent

The invention provides a transfection reagent based on blank lipid nanoparticles as well as a preparation method and application of the transfection reagent, and belongs to the technical field of biological medicines. The transfection reagent based on the blank lipid nanoparticles comprises the following components: (1) the blank lipid nanoparticles; (2) a biologically active ingredient; the blank lipid nanoparticles comprise ionizable lipid, phospholipid, cholesterol and polyethylene glycol conjugated lipid. The preparation process of the blank lipid nanoparticles and the transfection reagent is simple, and the preparation can be completed without the help of equipment. The transfection reagent based on the blank lipid nanoparticles is prepared from the blank lipid nanoparticles and nucleic acid, the dosage can be flexibly adjusted according to the requirements of a user, the transfection effect is stable, various cells (such as 293T, Hela, HepG2, TWO3 and MCF7) can be transfected, the cytotoxicity is low, and the transfection effect is good.
Owner:SCINDY PHARM (SUZHOU) CO LTD

Naphthoquinone compound in radix arnebiae seu lithospermi as well as preparation method and application of naphthoquinone compound in preparation of medicine for treating cervical cancer

The invention relates to the technical field of separation and purification of radix arnebiae seu lithospermi, in particular to a naphthoquinone compound in radix arnebiae seu lithospermi, a preparation method of the naphthoquinone compound and application of the naphthoquinone compound in preparation of drugs for treating cervical carcinoma, the naphthoquinone compound in radix arnebiae seu lithospermi is chemically named as (Z)-2-ethoxy-5, 8-dihydroxy-3-(4-methyl-1, 3-pentadiene-1-yl) naphthalene-1, 4-diketone, and the structural formula of the naphthoquinone compound is shown in the description. The naphthoquinone compound in the lithospermum is disclosed for the first time, in-vitro anti-tumor pharmacodynamic experiments are carried out on the naphthoquinone compound in the lithospermum, and the experiments show that the naphthoquinone compound in the lithospermum has a certain inhibition effect on human Hela cells; therefore, the naphthoquinone compound in the radix arnebiae seu lithospermi can be applied to preparation of drugs for preventing / treating cervical cancer.
Owner:PEOPLES HOSPITAL OF XINJIANG UYGUR AUTONOMOUS REGION

Tripterygium wilfordii exosome, preparation method and application of tripterygium wilfordii exosome in preparation of medicine for treating cervical tumor

The invention discloses application of a tripterygium wilfordii exosome in preparation of an anti-cervical cancer medicine and a tumor angiogenesis inhibiting medicine, and relates to the field of biological medicine. The medicinal plant exosome derived from tripterygium wilfordii is successfully separated, and it is proved that the medicinal plant exosome can regulate related pathways through delivery of functional nucleic acid molecules to inhibit proliferation and migration of cervical cancer cells and promote active oxygen related apoptosis so as to be used for tumor treatment. The tripterygium wilfordii exosome can further act on vascular endothelial cells in a tumor microenvironment, the migration function of Hela cells is inhibited, and then the effect of resisting cell proliferation in the tumor microenvironment is achieved. The tripterygium wilfordii exosome has the advantages of being simple in preparation method, remarkable in tumor growth resistance and tumor cell migration inhibition effect, good in biocompatibility, high in delivery efficiency and the like, and can be used as a novel nano-drug for tumor treatment.
Owner:QUFU NORMAL UNIV

Cervical cancer cell early screening and intelligent evaluation system based on multi-modal data

The invention relates to the technical field of medical information processing, in particular to a cervical cancer cell early screening and intelligent evaluation system based on multi-modal data, which comprises a data acquisition module, a form detection module and a screening early warning module, the data acquisition module is used for acquiring multi-modal data of a current detection object in a plurality of inspection processes; the morphology detection module is used for calculating a cellular morphology score of a current detection object in any target inspection process; the screening early warning module is used for determining similar detection objects of the current detection object, and correcting differences between the current detection object and the similar detection objects in the aspects of cellular morphology scores and lesion detection indexes according to the approximation degree between different types of lesion detection indexes of the current detection object; and obtaining the screening early warning coefficient of the current detection object by using the relative change condition of the correction result. According to the invention, the early screening and evaluation effects on cervical cancer cells are improved.
Owner:HUNAN LAIBOSAI MEDICAL ROBOT CO LTD +1

Five-membered sulfur-containing heterocyclic nucleoside lead compound and application thereof in resisting cervical cancer and pancreatic cancer activity

The invention discloses a five-membered sulfur-containing heterocyclic nucleoside lead compound and application thereof in resisting cervical cancer, pancreatic cancer and other activities, and belongs to the technical field of medicinal chemistry. A series of five-membered sulfur-containing heterocyclic ring nucleoside compounds are synthesized through a two-step Michael addition reaction, and the five-membered sulfur-containing heterocyclic ring nucleoside compounds comprise a racemate, (3S, 4R) and (3R, 4S): # imgabs0 # (* is a chiral center). Results show that in in-vitro cervical cancer (HeLa), pancreatic cancer (PANC-1) and other cell tests, the anti-tumor activity of the racemate is close to that of the enantiomer configuration. Wherein the chiral five-membered sulfur-containing heterocyclic nucleoside lead compound (3R, 4S)-15ab shows relatively strong proliferation inhibition capacity in a cervical cancer cell line, and IC50 (half maximal inhibitory concentration) reaches 2.78 mu M and is obviously superior to that of control drugs 5-fluorouracil and cis-platinum (IC50 is 9.75 mu M and 7.99 mu M respectively).
Owner:HENAN NORMAL UNIV

A pentacyclic thiazolyl indolinone piperazine amide derivative and uses thereof

PendingCN122444757ACarbamateO-Phosphoric Acid
The present application relates to a kind of five-ring thiazole indole ketone piperazine amide derivatives and purposes thereof.The derivatives take ethyl cyanoacetate as starting material, generate hydroxylamine compound (A) under the action of sodium nitrite and phosphoric acid;Obtain 2-amino ethyl cyanoacetate (B) by reduction, in turn with acetic anhydride, lawson reagent is reacted, and 5-amino-4-carboxylate thiazole compound (D) is obtained;After bromination by NBS, under the catalysis of phosphorus oxychloride, react with tetrahydropyridine indole ketone, generate 2-bromo-6,7-dihydrothiazolo [5'',4'':4',5'] pyrimido [1',2':1,2] pyrindo [3,4-b] indole-4 (12H) -ketone (F), again under alkaline condition, first with Boc piperazine, then by Boc treatment and obtain compound (H);Finally, react with acyl chloride, and 28 different substitution structures of five-ring thiazole indole ketone piperazine amide compound (I1-I28) are synthesized.The 28 compounds are tested on three kinds of cancer cells, and the results show that: 28 compounds have significant inhibitory activity on Hela cervical cancer cells, HT-29 human colon cancer cells and HGC-27 human gastric cancer cells.
Owner:XINJIANG INST OF ENG

Aza base [3,2-b] indole derivatives, processes for their preparation and use

This invention belongs to the field of organic synthesis and relates to a nitrogen-containing [3,2-b]indole derivative, its preparation method, and its application. The nitrogen-containing [3,2-b]indole derivative is a compound, optical isomer, or pharmaceutically acceptable salt thereof, as shown in the following structure: ; wherein R1, R2, R3, and R4 are independently selected from hydrogen atoms, halogens, cyano groups, C1-C8 alkyl groups, and C1-C8 alkoxy groups; R5, R6, R7, and R8 are independently selected from hydrogen atoms, halogens, and C1-C8 alkyl groups; R9 is selected from C1-C8 alkyl groups; when R1, R2, R3, R4, R5, R6, R7, and R8 are all hydrogen atoms, R9 is selected from C1-C2 alkyl groups. The compound exhibits antitumor activity, particularly against HeLa cervical cancer, showing a significant inhibitory effect on its proliferation.
Owner:CHANGSHA MEDICAL UNIV

N, N-diphenyl aniline compound with naphtho-indolizino-phenothiazine skeleton and preparation method and application of N, N-diphenyl aniline compound

The invention belongs to the field of organic synthesis and medicinal chemistry, and particularly provides an efficient synthesis method of an N, N-diphenyl aniline compound based on a naphtho-indolizino-phenothiazine skeleton and anti-tumor application of the N, N-diphenyl aniline compound based on the naphtho-indolizino-phenothiazine skeleton. Through Suzuki reaction, functional coupling based on a naphtho-indolizino-phenothiazine skeleton and an N, N-diphenyl aniline group is realized for the first time. In-vitro anti-tumor evaluation shows that the compound has remarkable inhibitory activity on various human tumor cells, especially has the strongest effect on breast cancer MCF-7 cells (IC50 = 0.15 mu M), and the activity is improved by 266 times compared with that of cis-platinum; prostate cancer PC-3, liver cancer HepG2, lung adenocarcinoma A549 and cervical cancer Hela cells are also remarkably inhibited. The toxicity to normal umbilical vein endothelial cells (HUVEC) is far lower than that of tumor cells, and the selectivity is excellent. The research provides a lead compound with great potential for developing high-efficiency and low-toxicity targeted anti-tumor drugs.
Owner:NANJING FORESTRY UNIV

Preparation method and application of tridentate clamp type metal iridium complex

The invention discloses a preparation method and application of a tridentate metal iridium complex, the preparation method of the tridentate metal iridium complex comprises the following steps: step 1, substituted 1, 3-benzene diformate and 2-aminothiophenol are subjected to cyclization reaction to obtain a first intermediate; 2, reacting iridium trichloride hydrate with the first intermediate obtained in the step 1 to obtain a second intermediate; and step 3, reacting an LX ligand with the second intermediate obtained in the step 2, and then using silver trifluoromethanesulfonate to obtain a target product. The tridentate clamp type metal iridium complex disclosed by the invention is composed of a substituted-1, 3-bis (benzothiazolyl) benzene main ligand, a 2, 2-dipyridyl or phenanthroline NN ligand and balanced chloride ions. The complex is simple in synthesis method and has high cytotoxicity to cervical cancer cells, colon cancer cells and lung cancer cells, and the in-vitro cell toxicity of the complex is obviously superior to that of clinically applied anti-tumor drug cis-platinum, so that the complex has a good application prospect in the field of metal anti-cancer drugs.
Owner:HAINAN NORMAL UNIV

1, 3, 4-oxadiazino tetrahydroisoquinoline compound as well as preparation method and application thereof

The invention provides a 1, 3, 4-oxadiazino tetrahydroisoquinoline compound as well as a preparation method and application thereof, and belongs to the technical field of heterocyclic compounds for medicines. The method comprises the following steps: by taking an azomethine imine substrate and a styrene oxide substrate as raw materials and cobalt perchlorate hexahydrate as a catalyst, adding the raw materials and the catalyst into a reaction solvent, reacting overnight at normal temperature, and performing column separation to obtain the 1, 3, 4-oxadiazino tetrahydroisoquinoline compound. According to the application, the reaction condition is mild, the selectivity is high, excellent cytotoxicity is shown on HeLa cervical cancer cells and A549 lung cancer cells, the half death inhibition ratio (IC50) value on tumor cells reaches the nanomole level, and the application has a good anti-cancer drug application prospect.
Owner:SHAOXING UNIVERSITY

New application of Edwardsiella fish-sourced protein EseO or coding gene thereof

PendingCN120661629AMetabolism disorderPeptide/protein ingredientsBiotechnologyEdwardsiella piscicida
The invention relates to an application of Edwardsiella fish-sourced protein EseO or a coding gene thereof in preparation of medicines for treating and / or preventing obesity. The edwardsiella fish source protein EseO screened by the invention can inhibit lipid metabolism of cells HeLa and mice C57 / BL6J, which proves that the edwardsiella fish source protein EseO has an obvious fat reducing effect and can be applied to feed additives, medical products and the like in the aquaculture industry related to weight loss.
Owner:EAST CHINA UNIV OF SCI & TECH