BIOMAT Database Logo BIOMAT Database Logo

Design, synthesis and antitumor activity of novel artemisinin derivatives using hybrid approach. 2011

Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Japan.

In an attempt to develop potent and selective anti-tumor agents, two novel series of artemisinin-chalcone hybrids were designed, synthesized and screened for their antitumor activities against HT-29, A549, MDA-MB-231, HeLa and H460 cell lines in vitro. Nearly all of the tested compounds showed significantly increased anti-tumor activity compared with the corresponding dihydroartemisinin (DHA). Most of the title compounds displayed good selectivity toward HT-29 and HeLa cell lines with IC₅₀ values ranging from 0.09 to 0.85 µM. Among them, the most promising compound 9c (IC₅₀) range of 0.09-0.93 µM) was 10.5- to 70-times more active than DHA (IC₅₀ range of 5.6-15.6 µM) respectively.

UI MeSH Term Description Entries
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D009369 Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms. Benign Neoplasm,Cancer,Malignant Neoplasm,Tumor,Tumors,Benign Neoplasms,Malignancy,Malignant Neoplasms,Neoplasia,Neoplasm,Neoplasms, Benign,Cancers,Malignancies,Neoplasias,Neoplasm, Benign,Neoplasm, Malignant,Neoplasms, Malignant
D002599 Chalcone An aromatic KETONE that forms the core molecule of CHALCONES. Benzalacetophenone,Benzylideneacetophenone,1,3-Diphenyl-2-Propen-1-One,Chalkone,1,3 Diphenyl 2 Propen 1 One
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
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000972 Antineoplastic Agents, Phytogenic Agents obtained from higher plants that have demonstrable cytostatic or antineoplastic activity. Antineoplastics, Botanical,Antineoplastics, Phytogenic,Agents, Phytogenic Antineoplastic,Botanical Antineoplastics,Phytogenic Antineoplastic Agents,Phytogenic Antineoplastics
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
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
D018360 Crystallography, X-Ray The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) X-Ray Crystallography,Crystallography, X Ray,Crystallography, Xray,X Ray Crystallography,Xray Crystallography,Crystallographies, X Ray,X Ray Crystallographies

Related Publications

Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, Synthesis, and Antitumor Activity of Novel Quinazoline Derivatives.
September 2017, Molecules (Basel, Switzerland),
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, Synthesis, and Antitumor Activities of Isomers of Artemisinin Dimer Derivatives.
July 2023, Chemistry & biodiversity,
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, Synthesis, and Antitumor Activity Evaluation of Artemisinin Bivalent Ligands.
January 2024, Molecules (Basel, Switzerland),
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, synthesis and antitumor activity of novel D-glucuronic acid derivatives.
November 2011, Medicinal chemistry (Shariqah (United Arab Emirates)),
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Synthesis and antimalarial activity of novel dihydro-artemisinin derivatives.
May 2011, Molecules (Basel, Switzerland),
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Synthesis and anticancer activity of novel aza-artemisinin derivatives.
July 2017, Bioorganic & medicinal chemistry,
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.
October 2017, Bioorganic & medicinal chemistry,
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, synthesis and antitumor activity of icotinib derivatives.
December 2020, Bioorganic chemistry,
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, Synthesis, and Antitumor Activity of Erlotinib Derivatives.
January 2022, Frontiers in pharmacology,
Lijun Xie, and Xin Zhai, and Lixiang Ren, and Haiyan Meng, and Chun Liu, and Wufu Zhu, and Yanfang Zhao
Design, synthesis and antitumor evaluation of novel celastrol derivatives.
July 2019, European journal of medicinal chemistry,
Copied contents to your clipboard!