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120 results about "Nsclc cell" patented technology

Alkaloid compound as well as preparation method and anti-tumor application thereof

The invention provides an alkaloid compound as well as a preparation method and an application thereof in tumor resistance. The alkaloid compound provided by the invention shows a remarkable cytotoxic effect on human non-small cell lung cancer cells A549, mouse lung adenocarcinoma cells Lewis, human triple negative breast cancer cells MDA-MB-231 and mouse breast cancer cells 4T1, and can be used for preparing medicines for treating breast cancer, lung cancer and the like.
Owner:CHINESE MEDICINE GUANGDONG LABORATORY +1

Coumarin KRAS-G12C inhibitor as well as preparation and application thereof

The invention discloses a coumarin KRAS-G12C inhibitor as well as preparation and application of the coumarin KRAS-G12C inhibitor. The coumarin compound disclosed by the invention has a remarkable inhibition effect on non-small cell lung cancer cells (NCI-H23 and NCI-H358) with high expression of KRAS-G12C and pancreatic cancer cells (MIAPaCa-2), is particularly used for preparing medicines for treating and / or preventing non-small cell lung cancer and pancreatic cancer, and has a good prospect of development and application of antitumor medicines.
Owner:LANZHOU UNIV

Application of copper death inducer in preparation of medicine for treating osimertinib-resistant non-small cell lung cancer

The invention provides application of a copper death inducer in preparation of a medicine for treating osimertinib-resistant non-small cell lung cancer, and belongs to the technical field of treatment of non-small cell lung cancer. According to the invention, through high-throughput drug screening, the copper death inducer copper diethyl dithiocarbamate (CuET) and osimertinib are combined for use, so that a remarkable synergistic anti-cancer effect is achieved; furthermore, through detection of a wild type and osimertinib drug-resistant cell line model, an osimertinib sensitive and drug-resistant patient-derived organoid and a mouse xenotransplantation model, it is found that the anti-tumor effect of osimertinib can be remarkably enhanced through copper death induction, and osimertinib drug resistance is overcome. According to the technical scheme provided by the invention, osimertinib drug-resistant non-small cell lung cancer cells can be effectively killed, the curative effect of osimertinib in sensitive and drug-resistant models is remarkably enhanced, and an application scene is provided for copper death in tumor treatment.
Owner:CANCER INST & HOSPITAL CHINESE ACADEMY OF MEDICAL SCI

SOD2 knockout cell line and application thereof in anti-poxvirus

The invention discloses an SOD2 knockout cell line and application of the SOD2 knockout cell line in anti-poxvirus, and relates to the technical field of antiviral research. According to the invention, sgRNA of targeted superoxide dismutase 2 (SOD2) is designed, the sequence of the sgRNA is shown as SEQ ID NO.1-SEQ ID NO.2, then a stable SOD2 knockout human-derived non-small cell lung cancer A549 cell line is established by combining CRISPR / Cas9 gene editing with a lentiviral vector delivery technology, single-cell cloning is obtained through multiple rounds of puromycin screening, and the SOD2 gene knockout A549 cell strain is successfully constructed. Vaccinia virus Tian Tan strain infection shows that the number of plaques of SOD2 knockout cells is obviously greater than that of the plaques (about 2.3 times) of normal cell infection, and the plaques are relatively large, so that fine SOD2 has the effect of limiting intercellular transmission of poxvirus. The invention lays a foundation for research and preparation of antiviral drugs.
Owner:INST OF ANIMAL HEALTH GUANGDONG ACADEMY OF AGRI SCI

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

Actinomycetes-derived polyketone compound as well as preparation method and application thereof

The invention discloses a polyketone compound derived from actinomycetes as well as a preparation method and application thereof, and relates to the technical field of microbial natural product mining and biological medicine, and the key point of the technical scheme is that the invention discloses a novel polyketone compound Strepactone derived from actinomycetes Streptomyces sp. DP0001, and the molecular formula of the novel polyketone compound Strepactone is C25H38O5. The compound is obtained through strain fermentation, ethyl acetate extraction and multi-step chromatographic purification, and the structure is identified through ESI-MS, 1H NMR and 13C NMR. Experiments show that Strepactone has an inhibition effect on staphylococcus aureus and methicillin-resistant staphylococcus aureus and has remarkable inhibition activity on human non-small cell lung cancer A549 cells, the half inhibitory concentration IC50 of the Strepactone is 5.36 mu M, and the Strepactone has no obvious cytotoxic activity on human embryo kidney cells 293T cells at the concentration of 30 mu M. The compound provided by the invention can be used for preparing anti-drug-resistant bacteria drugs and anti-human non-small cell lung cancer drugs, and also provides a structural basis for the development of novel antibacterial and anti-tumor leading drugs.
Owner:GUIZHOU MEDICAL UNIV

Preparation and application of novel pyrimidine KRAS G12C inhibitor

The invention discloses a novel pyrimidine KRAS-G12C inhibitor as well as a preparation method and application of the novel pyrimidine KRAS-G12C inhibitor. The pyrimidine compound disclosed by the invention has a remarkable inhibition effect on non-small cell lung cancer cells (NCI-H23 and NCI-H358) with high expression of KRAS-G12C, is particularly used as a medicine for treating and / or preventing the non-small cell lung cancer, is simple and efficient in preparation route, and has a good antitumor medicine development and application prospect.
Owner:LANZHOU UNIV

Use of raltitrexed in the manufacture of a medicament for the treatment of a disease caused by an adenovirus infection

ActiveCN120983440BEnhanced inhibitory effectImprove pathological conditionsOrganic active ingredientsAntiviralsRaltitrexedCancer research
The present application provides the use of raltitrexed in the manufacture of a medicament for the treatment of diseases caused by adenovirus infection, including but not limited to respiratory tract infection, gastrointestinal infection and keratitis caused by adenovirus. When raltitrexed was tested for its anti-adenovirus activity at the cellular level, using a viral infection dose of 100 TCID50, the viral infectivity was determined on a human non-small cell lung cancer cell line (A549 cell) model, and the results showed that raltitrexed had a significant inhibitory effect on adenovirus, with an EC 50 = 8.98 nM, a CC 50 > 187.5 nM, and it was found that it had a significant inhibitory effect on the entry of the virus into the cell; and in the hDSG2 mouse model, a significant inhibitory effect of raltitrexed on viral replication was also observed. Therefore, raltitrexed can be used to treat diseases caused by adenovirus infection.
Owner:BEIJING UNIV OF CHEM TECH

Preparation method and application of tetrahydroindazole antitumor compounds

The present application relates to the technical field of medicine (IPC classification A61P31 / 22), and particularly relates to a preparation method and application of a tetrahydroindazole antitumor compound, the preparation method comprising: reacting a compound of formula I with adamantanol to obtain a 4-(4-hydrazone-3,6,6-trimethyl-1-tetrahydroindazole)-2-(4-hydroxycyclohexylamino) benzamide compound, compared with a 4-(4-hydrazone-3,6,6-trimethyl-1-tetrahydroindazole)-2-(4-hydroxycyclohexylamino) benzamide compound in the prior art, the compound has stronger inhibition of tumor cell growth activity, has generally lower IC50 values, and in particular can significantly reduce the clonogenicity of non-small cell lung cancer at a low concentration, and causes apoptosis of non-small cell lung cancer cells, and has great significance for development of a novel antitumor drug.
Owner:SHENZHEN PEOPLES HOSPITAL

Application of 3 'tRF-mtAsnGTT inhibitor in preparation of medicine for treating osimertinib drug-resistant non-small cell lung cancer

The invention belongs to the field of gene engineering, and particularly designs oligonucleotide and application thereof in preparation of a medicine for treating osimertinib drug-resistant non-small cell lung cancer. Research finds that 3 'tRF-mtAsnGTT is highly expressed in osimertinib drug-resistant non-small cell lung cancer cells, and the inventor designs an effective oligonucleotide capable of specifically inhibiting the function of 3' tRF-mtAsnGTT, so that tumor cell proliferation is inhibited, cell apoptosis is promoted, and the drug sensitivity of the cells to osimertinib is remarkably improved. The invention provides a novel targeting strategy and application approach for molecular intervention and combined treatment of osimertinib resistance of non-small cell lung cancer.
Owner:THE SECOND AFFILIATED HOSPITAL OF NANJING MEDICAL UNIV

Application of LncRNA as non-small cell lung cancer biomarker and therapeutic target

The invention belongs to the technical field of biological medicine, and particularly relates to application of LncRNA as a non-small cell lung cancer biomarker and a treatment target spot, and the nucleotide sequence of the LncRNA is shown as SEQ ID NO. 1. Experimental results show that proliferation, survival and migration of non-small cell lung cancer cells can be prevented by inhibiting expression of the LncRNA, so that the LncRNA can be used as a non-small cell lung cancer biomarker and a therapeutic target.
Owner:ZHEJIANG UNIV

Agonist of retinoic acid receptor beta and application of agonist in preparation of non-small cell lung cancer medicine

The invention discloses an agonist of a retinoic acid receptor beta and application of the agonist in preparation of a non-small cell lung cancer medicine in the technical field of biological medicine. The agonist of the retinoic acid receptor beta is saturated odd fatty acid heptadecanoic acid C17: 0; according to the research, the expression of a retinoic acid receptor beta can be up-regulated by adding heptadecanoic acid into the NSCLC cells, so that the sensitivity of the NSCLC cells to retinoic acid treatment is improved. When heptadecanoic acid and retinoic acid are combined for use, the activity and migration ability of NSCLC cells can be further inhibited, and apoptosis of the cells is promoted. The result shows that the heptadecanoic acid plays an important role in controlling the sensitivity of the NSCLC cells to the retinoic acid, the combined use of the heptadecanoic acid and the retinoic acid provides a new drug treatment means for treating the NSCLC, and the heptadecanoic acid and the retinoic acid have potential application value in preparing the drug for treating the non-small cell lung cancer.
Owner:ANHUI UNIV

Nucleotide for inhibiting expression of ILKAP related circular RNA (Ribonucleic Acid) and application of nucleotide

The invention discloses a nucleotide for inhibiting expression of ILKAP (Interleukin-7-Kinase Associated Protein) related circular RNA (Ribonucleic Acid) and application of the nucleotide, and the nucleotide is characterized in that the nucleotide sequence is CGUCAGUACUCGGGUUUCA, and the expression level of hsacirc0001116 can be specifically and obviously reduced. Experimental results prove that the nucleic acid molecule can effectively interfere with the expression of hsacirc0001116 in human non-small cell lung cancer A549 cells, and can significantly inhibit the survival of lung cancer cells. In addition, when the nucleic acid molecule is combined with an existing antitumor drug for use, a synergistic treatment effect can be generated.
Owner:KUNMING MEDICAL UNIVERSITY

Ruthenium complex for inducing mitochondrial DNA polycondensation to overcome tumor drug resistance, anti-tumor drug and preparation method and application thereof

The invention discloses a ruthenium complex for inducing mitochondrial DNA polycondensation to overcome tumor drug resistance, an anti-tumor drug and a preparation method and application of the ruthenium complex and the anti-tumor drug. The ruthenium complex is connected with a triphenylphosphine structure-modified bipyridine diazo-anthracene ligand through an alkyl chain, so that the fat solubility of the complex is improved, and the complex can enter cells more easily; the complex has a mitochondrial enrichment function and can be enriched in mitochondria; the complex induces mitochondrial DNA polycondensation so as to cause cancer cell death; the targeting property on tumor cells is effectively improved; the IC50 of the compound on human non-small cell lung cancer cell strains and cis-platinum drug-resistant strains thereof is far lower than that of cis-platinum, and the compound can be used as an excellent anti-tumor drug. The complex takes a ruthenium-coordinated ruthenium precursor compound as a raw material, and the raw material is economical and easy to obtain; the selectivity of the ruthenium complex can be improved, and the cost is saved.
Owner:GUANGDONG UNIV OF TECH

A fuzheng sanjie recipe for resisting non-small cell lung cancer and a preparation method thereof

The present application relates to a kind of anti-non-small cell lung cancer for strengthening healthy qi and resolving stasis and preparation method thereof, strengthening healthy qi and resolving stasis is made from the following weight proportion of raw medicinal materials: Ficus pumila 2g~50g / portion, radix pseudostellariae 2g~50g / portion, poria cocos 2g~50g / portion, atractylodes 2g~50g / portion, radix scutellariae 2g~50g / portion, oldenlandia 2g~50g / portion, cat's paw grass 2g~50g / portion, giant knotweed 2g~50g / portion, curcuma zedoary 2g~50g / portion, oyster 2g~50g / portion, platycodon 2g~50g / portion, mountain bitterling 2g~50g / portion, half branch orchid 2g~50g / portion. By cell test and the construction NSCLC osimertin drug resistance animal model prove, strengthening healthy qi and resolving stasis of the present application can adjust tumor microenvironment (TME) and inhibit non-small cell lung cancer cell growth of osimertin drug resistance. Not only this, strengthening healthy qi and resolving stasis of the present application can also inhibit common non-small cell lung cancer cell growth. While clinical observation finds, strengthening healthy qi and resolving stasis of the present application can improve insomnia, skin rash, diarrhea and other symptoms of lung accumulation (lung cancer, lung nodule) patient, improve its quality of life.
Owner:SHENZHEN BAOAN DISTRICT TRADITIONAL CHINESE MEDICINE HOSPITAL

Method of using AC electric fields and checkpoint inhibitors

A method for improving the survival of a subject with cancer is disclosed, comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more cancer cells for a predetermined period of time, and administering the subject a therapeutically effective amount of a checkpoint inhibitor. A method for treating a subject with cancer is disclosed, comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more cancer cells for a predetermined period of time, and administering the subject a therapeutically effective amount of a checkpoint inhibitor. In some embodiments, the checkpoint inhibitor is nivolumab, pembrolizumab, or atezolizumab. Furthermore, a method for improving the survival of a subject with non-small cell lung cancer is disclosed, comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more non-small cell lung cancer cells for a predetermined period of time, and administering the subject a therapeutically effective amount of a checkpoint inhibitor. A method for treating a subject having non-small cell lung cancer is disclosed, the method comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more non-small cell lung cancer cells for a predetermined period of time, and administering to the subject a therapeutically effective amount of a checkpoint inhibitor. In some embodiments, the checkpoint inhibitor is ipilimumab (Yervoy), pembrolizumab (Keytruda), nivolumab (Opdivo), semiprimab (brand name Ributayo), dostallimab (Jemperli), atezolizumab (Tecentriq), durvalumab (Imfinzi), or avelumab (Bavencio).
Owner:NOVOCURE GMBH CH

Aspirin-sulfonamide hybrids, processes for their preparation and use

The application relates to the technical field of aspirin pharmaceutical chemistry, in particular to an aspirin-sulfonamide hybrid, a preparation method and application thereof. The preparation method can synthesize a plurality of novel aspirin-sulfonamide hybrids by taking piperazine as a bridge, and by a three-step continuous method of "acyl chlorination, sulfonamidation and N-acylation" according to a "molecular hybridization principle". In the process, only one separation and purification is performed, and the preparation steps are simple. The aspirin-sulfonamide hybrid prepared by the method is most effective on human non-small cell lung cancer cells A549, and the activity is more than 33 times higher than that of a parent aspirin, and is similar to the activity of an anticancer drug irinotecan. The aspirin-sulfonamide hybrid 3k prepared by the method has a certain inhibitory effect on various cancer cells. The hybrid can induce human non-small cell lung cancer A549 cell apoptosis in a concentration-dependent manner, and can induce human non-small cell lung cancer A549 cell cycle arrest in the G0 / G1 phase, and inhibit cell growth.
Owner:NINGXIA UNIVERSITY

Novel beta-carboline quaternary salt derivatives, methods of making and using the same

This invention discloses a novel class of β-carboline quaternary ammonium salt derivatives, their preparation methods, and applications. The derivatives have the structure shown in Formula I, where R1, R2, and R3 are various substituents, and X... ‑ It is a halide ion. Its preparation method uses substituted indole-2-methylamine and substituted α-haloacetophenone as starting materials, and constructs them through a one-step cyclization reaction in an aprotic solvent mediated by a catalytic protic acid (such as p-toluenesulfonic acid). This method is mild, simple to operate, requires no metal catalyst, eliminates the risk of metal residue, and has good functional group compatibility. Activity tests of the obtained series of compounds showed that they have significant inhibitory activity against the proliferation of non-small cell lung cancer cell lines (such as A549 and H1299), with some compounds exhibiting activity superior to the positive control drug cisplatin. Therefore, this compound has important application value in the preparation of antitumor drugs, especially anti-lung cancer drugs.
Owner:TAIZHOU VOCATIONAL & TECHN COLLEGE

Simple preparation process of semi-sandwich ruthenium triphenyl phosphine dithioformic acid complex and application thereof

PendingCN122356164AMorpholineIn vitro test
This invention discloses a semi-sandwich structured ruthenium triphenylphosphine dithiocarboxylic acid complex with a simple preparation process and its applications. The complex has the structure shown in Figure (I), with the central ruthenium and... η 5 - Coordination with cyclopentadiene, triphenylphosphine, and dithiocarboxylic acid derivatives, wherein the dithiocarboxylic acid ligands are selected from ethyl xanthic acid, isopropyl xanthic acid, ... N,N Diethyldithiocarbamic acid, morpholine dithiocarbamic acid, and carbazole dithiocarbamic acid. This invention employs a simple one-step method of room temperature preparation and recrystallization purification using a ruthenium precursor and dithiocarbamic acid ligand. This method offers advantages such as readily available raw materials, mild reaction conditions, simple post-processing, and high yield. In vitro tests show that the complexes exhibit excellent anti-proliferative activity against non-small cell lung cancer A549 cells, significantly superior to cisplatin. The complexes demonstrate activity by reducing mitochondrial membrane potential, inducing intracellular reactive oxygen species accumulation, and arresting the cell cycle (G1 phase), leading to late apoptosis in A549 cells.
Owner:QUFU NORMAL UNIV

Use of ppb in the preparation of a drug for preventing or treating non-small cell lung cancer

PendingCN122351427AOncologyH1299 cell
The application provides an application of PPB in preparation of a drug for preventing or treating non-small cell lung cancer, and relates to the technical field of biological medicines. TRIM47 The CAS number of the PPB is 1415504-32-3. The PPB provided in the application can effectively inhibit the migration and activity of NCI-H1299 cells and SPC-A1 cells, two kinds of non-small cell lung cancer cells, thereby helping to provide a safer and more effective treatment scheme for non-small cell lung cancer treatment.
Owner:NANCHANG UNIV

Natural fissistilarin component derivative DhpB and application thereof

The application discloses a natural fissistilarin component derivative DhpB and application thereof, and particularly application thereof as a covalent binding ubiquitinase MKRN2 target in anti-KRAS mutant lung cancer. The derivative is from a plant of Peperomia in Piperaceae, can significantly inhibit in-vivo and in-vitro proliferation of KRAS mutant non-small cell lung cancer cells, and induce tumor cell apoptosis through semi-synthetic structure optimization. DhpB is covalently combined with ubiquitinase MKRN2 abnormally expressed in KRAS mutant lung cancer cells, promotes combination of MKRN2 and small ribosomal protein RPS7, thereby promoting ubiquitination and degradation of RPS7, and causes ribosome stress-induced apoptosis of tumor cells. The application provides a new target and inhibitor for preparing a drug for treating refractory KRAS mutant lung cancer, and has a good medicinal prospect.
Owner:NANJING UNIV OF TRADITIONAL CHINESE MEDICINE

Application of berberine in preparation of medicine for treating non-small cell lung cancer

The invention discloses application of berberine in preparation of a medicine for treating non-small cell lung cancer, and belongs to the technical field of biological medicine. The invention provides an application of berberine in preparation of a medicine for inhibiting or treating EGFR (epidermal growth factor receptor) driven diseases, or an application of berberine combined with other medicines in preparation of a medicine for inhibiting or treating EGFR driven diseases. The diseases comprise non-small cell lung cancer driven by EGFR (epidermal growth factor receptor). It is found that in PC-9 cells, berberine induces ROS accumulation and starts a mitochondrial injury pathway, then mitochondrial membrane potential is reduced, GSDME is activated to form an active N-terminal fragment (GSDME-N), then pyroptosis is induced, NSCLC cell proliferation is inhibited, and berberine is expected to overcome or delay EGFR TKI drug resistance and improve clinical effects and survival prognosis.
Owner:HEFEI INSTITUTE OF PHYSICAL SCIENCE CHINESE ACADEMY OF SCIENCES

A phloroglucinol derivative having antitumor activity and a preparation method and application thereof

This invention belongs to the technical field of chemical pharmaceuticals, specifically relating to a phloroglucinol derivative with antitumor activity, its preparation method, and its applications. The preparation involves adding acyl-phloroglucinol compounds and amine compounds to an organic solvent under amine catalysis, reacting at room temperature, and purifying to obtain a series of phloroglucinol derivatives. The phloroglucinol derivatives formed in this invention, in addition to retaining the phloroglucinol core, have other groups with potential antitumor activity linked through imine groups, exhibiting a novel structure and good antitumor activity. They show excellent anti-proliferative effects against human non-small cell lung cancer cells A549 and have broad application prospects.
Owner:GUANGDONG PHARMA UNIV

A small molecule fluorescent photosensitizer containing a gefitinib backbone structure and an AIE group, its preparation and application

This invention relates to a small-molecule fluorescent photosensitizer containing a gefitinib backbone structure and an AIE group, its preparation, and its application, belonging to the field of fluorescent photosensitizer technology. The fluorescent photosensitizer includes an AIE group, a linking group, and a recognition group. On one hand, the AIE group backbone structure consists of a pyridine cation (electron acceptor, A), an ethylene group (π-bridge), a thiophene fragment (π-bridge and electron donor, D), and a triphenylamine segment (D), which is a typical D-π-A molecular configuration, thus exhibiting near-infrared fluorescence emission. On the other hand, by introducing heavy atoms to enhance the spin-orbit coupling of the photosensitizer, the efficiency of singlet oxygen generation is improved. The fluorescent photosensitizer can precisely target EGFR-overexpressing non-small cell lung cancer cells without illuminating normal cells. The fluorescent photosensitizer exhibits aggregation-induced emission properties, avoiding the ACQ effect during aggregation, greatly improving the ROS generation efficiency and promoting its tumor-killing effect.
Owner:BEIJING INST OF TECH

A compound based on the structure of 6-methylfurano[2,3-d]pyrimidine-4(3H)-one, its preparation method and application

This invention belongs to the field of pharmaceutical synthesis technology, specifically relating to a compound based on the 6-methylfurano[2,3-d]pyrimidine-4(3H)-one structure, its preparation method, and its applications. The compound provided by this invention, based on the 6-methylfurano[2,3-d]pyrimidine-4(3H)-one structure, enhances the chelation effect between the compound and zinc ions in histone deacetylases by combining the pharmacophore of a DNA methyltransferase 3A inhibitor with an isohydroxamic acid fragment, thus exhibiting strong HDAC inhibitory activity while maintaining DNMT3A inhibition. The compound provided by this invention shows significantly higher inhibitory activity against human non-small cell lung cancer cells H460 than against H460 DNMT3A-HDAC6 double knockout cells, demonstrating in vivo activity against human non-small cell lung cancer and possessing application value as a therapeutic agent for diseases and disorders related to DNMT3A and HDAC6.
Owner:SHENYANG PHARMA UNIV

Third-generation ALK TKI drug loratinib-resistant cell strain as well as construction method and application thereof

The invention relates to the technical field of biomedicine, in particular to a third-generation ALK TKI drug loratinib drug-resistant cell strain as well as a construction method and application thereof, the drug-resistant cell strain is a loratinib-resistant human non-small cell lung cancer cell strain H3122 LS and is preserved in Guangdong Microbial Culture Collection Center on July 25, 2025, and the preservation number is GDMCC No: 66760. According to the invention, an EML4-ALK fusion driven H3122 cell is treated by using a third generation of ALK TKI loratinib, a cell with high drug resistance to loratinib is formed through induction, and it is found that the drug-resistant cell loses EML4-ALK fusion variation. At present, the drug-resistant mechanism of the ALK inhibitor is not clarified clinically, and the construction of the drug-resistant cell and the discovery of the drug-resistant mechanism are beneficial to guiding clinical discovery of a new potential drug-resistant mechanism; a new drug-resistant related driver gene or signal pathway is found, and an experimental basis is provided for subsequent treatment strategy selection of a drug-resistant patient.
Owner:SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV

Preparation of a 10-trifluoromethoxycamptothecin derivative and its use in antitumor therapy

This invention relates to the preparation of 10-trifluoromethoxycamptothecin compounds and their use in antitumor drugs. The structural formula of these compounds is shown below. In vitro cytotoxicity screening results show that 10-trifluoromethoxycamptothecin compounds possess broad-spectrum antitumor activity, exhibiting strong inhibitory activity against human hepatocellular carcinoma cells (HepG2), human non-small cell lung cancer cells (A549), human colon cancer cells (SW480), human cholangiocarcinoma cells (QBC939), human breast cancer cells (MCF-7), human pancreatic cancer cells (PANC-1), and human pancreatic cancer cells (BxPC-3). Compounds 10-trifluoromethoxycamptothecin I and 7-ethyl-10-trifluoromethoxycamptothecin II showed strong inhibitory effects against all seven tested tumor cell lines, with IC50 values ​​exceeding 100%. 50 The concentrations were 0.913–0.0661 μM and 4.932–0.0578 μM, respectively, both significantly superior to the control drug topotecan. Among them, compounds I and II exhibited the strongest inhibitory activity against the BxPC-3 cell line, with IC50 values ​​of [missing value]. 50 The values ​​were 0.0661±0.0065μM and 0.0578±0.0043μM, respectively. Therefore, 10-trifluoromethoxycamptothecin compounds hold promise for development into a novel antitumor drug.
Owner:LANZHOU UNIV

Application of LncRNA as biomarker and therapeutic target for non-small cell lung cancer

The application belongs to the technical field of biological medicine, and particularly relates to application of LncRNA as a non-small cell lung cancer biomarker and treatment target, wherein the nucleotide sequence of the LncRNA is shown as SEQ ID NO. 1. Experimental results of the application show that inhibition of expression of the LncRNA can prevent proliferation, survival and migration of non-small cell lung cancer cells, and therefore the LncRNA can be used as a non-small cell lung cancer biomarker and treatment target.
Owner:ZHEJIANG UNIV

Preparation and application of novel magnolol and jateorhizine conjugate

The invention discloses preparation and application of a novel magnolol and jatrorrhizine conjugate, relates to the technical field of medicines, and aims to overcome the defects of poor drug resistance and insufficient activity of a single-target anti-cancer drug. According to the technical scheme, acetone or acetonitrile is used as a solvent, and through a two-step substitution reaction, the magnolol and jatrorrhizine conjugate is obtained; the preparation method comprises the following steps: reacting magnolol with dibromo-alkane to generate an intermediate B, and conjugating the intermediate B with jatrorrhizine to obtain a final product with a general formula C; or the jatrorrhizine reacts with dibromo alkane to generate an intermediate E, and then the intermediate E is conjugated with magnolol to obtain the final product of the general formula C. In the preparation process, reaction conditions (such as potassium carbonate alkaline environment and 82 DEG C reflux) are optimized, and high yield and purity are realized. The conjugate disclosed by the invention is widely applied to the anti-tumor field, has remarkable inhibitory activity on various cancer cells (such as non-small cell lung cancer cells HCC827 and human lung adenocarcinoma cells H1975), has better effects than magnolol and jateorhizine monomers, and provides a new candidate for research and development of multi-target drugs.
Owner:KAILI UNIV