BIOMAT Database Logo BIOMAT Database Logo

Design and synthesis of novel 2'-hydroxy group substituted 2-pyridone derivatives as anticancer agents. 2013

Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.

We have synthesized a series of novel 2-pyridone derivatives with 1,2,3-triazole and evaluated their anti-tumor activities in vitro. The bioassays showed that the majority of the resultant compounds exerted inhibitory effects on six human cancer cell lines to various extents. In particular, compound 10k showed the best anti-tumor activities (IC50 values of A549, HeLa and SW480 cancer cell lines were 0.86 ± 0.17 μM, 0.54 ± 0.23 μM and 0.21 ± 0.13 μM, respectively).

UI MeSH Term Description Entries
D011728 Pyridones Pyridine derivatives with one or more keto groups on the ring. Pyridinones
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004354 Drug Screening Assays, Antitumor Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals. Anticancer Drug Sensitivity Tests,Antitumor Drug Screens,Cancer Drug Tests,Drug Screening Tests, Tumor-Specific,Dye Exclusion Assays, Antitumor,Anti-Cancer Drug Screens,Antitumor Drug Screening Assays,Tumor-Specific Drug Screening Tests,Anti Cancer Drug Screens,Anti-Cancer Drug Screen,Antitumor Drug Screen,Cancer Drug Test,Drug Screen, Anti-Cancer,Drug Screen, Antitumor,Drug Screening Tests, Tumor Specific,Drug Screens, Anti-Cancer,Drug Screens, Antitumor,Drug Test, Cancer,Drug Tests, Cancer,Screen, Anti-Cancer Drug,Screen, Antitumor Drug,Screens, Anti-Cancer Drug,Screens, Antitumor Drug,Test, Cancer Drug,Tests, Cancer Drug,Tumor Specific Drug Screening Tests
D006367 HeLa Cells The first continuously cultured human malignant CELL LINE, derived from the cervical carcinoma of Henrietta Lacks. These cells are used for, among other things, VIRUS CULTIVATION and PRECLINICAL DRUG EVALUATION assays. Cell, HeLa,Cells, HeLa,HeLa Cell
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D045744 Cell Line, Tumor A cell line derived from cultured tumor cells. Tumor Cell Line,Cell Lines, Tumor,Line, Tumor Cell,Lines, Tumor Cell,Tumor Cell Lines

Related Publications

Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design, synthesis and bioevaluation of novel 6-substituted aminoindazole derivatives as anticancer agents.
December 2020, RSC advances,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design, synthesis and biological evaluation of 3-substituted-2-oxindole hybrid derivatives as novel anticancer agents.
July 2017, European journal of medicinal chemistry,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design, synthesis and anticancer evaluation of some novel 7-hydroxy-4-methyl-3-substituted benzopyran-2-one derivatives.
March 2024, Future medicinal chemistry,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design and synthesis of novel substituted quinazoline derivatives as antileishmanial agents.
September 2009, Bioorganic & medicinal chemistry letters,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design and synthesis of 2-phenylpyrimidine coumarin derivatives as anticancer agents.
October 2017, Bioorganic & medicinal chemistry letters,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Novel N-substituted sophoridinol derivatives as anticancer agents.
June 2014, European journal of medicinal chemistry,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design, synthesis and pharmacological evaluation of novel substituted quinoline-2-carboxamide derivatives as human dihydroorotate dehydrogenase (hDHODH) inhibitors and anticancer agents.
July 2014, European journal of medicinal chemistry,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design, synthesis and biological evaluation of novel pyrenyl derivatives as anticancer agents.
January 2015, European journal of medicinal chemistry,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Design, synthesis and evaluation of novel levoglucosenone derivatives as promising anticancer agents.
July 2020, Bioorganic & medicinal chemistry letters,
Zhiliang Lv, and Yikai Zhang, and Mingfeng Zhang, and Huan Chen, and Zhenliang Sun, and Dongping Geng, and Chunjuan Niu, and Ke Li
Antitumor agents 253. Design, synthesis, and antitumor evaluation of novel 9-substituted phenanthrene-based tylophorine derivatives as potential anticancer agents.
July 2007, Journal of medicinal chemistry,
Copied contents to your clipboard!