Bis-2(5H)-furanone derivatives as new anticancer agents: Design, synthesis, biological evaluation, and mechanism studies. 2018

Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
School of Chemistry and Environment, South China Normal University, Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, Guangzhou, China.

New bis-2(5H)-furanone derivatives containing a benzidine core were synthesized via a one-step transition-metal-free reaction of benzidine with 5-substituted 3,4-dihalo-2(5H)-furanones. Their antitumor activities against various tumor cells have been evaluated by MTT assay. Among them, compound 4e exhibits significant inhibitory activity against C6 glioma cells with an IC50 value of 12.1 μm and low toxicity toward HaCaT human normal cells. Studies on the antitumor mechanism reveal that cell cycle arrest at S-phase in C6 cells is induced by compound 4e. Furthermore, investigations with electronic, fluorescence emission and circular dichroism spectra show that compound 4e can significantly interact with C6-DNA. These data indicate that DNA may be one of the potential targets for bis-2(5H)-furanone derivatives as anticancer drugs.

UI MeSH Term Description Entries
D009690 Nucleic Acid Conformation The spatial arrangement of the atoms of a nucleic acid or polynucleotide that results in its characteristic 3-dimensional shape. DNA Conformation,RNA Conformation,Conformation, DNA,Conformation, Nucleic Acid,Conformation, RNA,Conformations, DNA,Conformations, Nucleic Acid,Conformations, RNA,DNA Conformations,Nucleic Acid Conformations,RNA Conformations
D002942 Circular Dichroism A change from planar to elliptic polarization when an initially plane-polarized light wave traverses an optically active medium. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Circular Dichroism, Vibrational,Dichroism, Circular,Vibrational Circular Dichroism
D004247 DNA A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine). DNA, Double-Stranded,Deoxyribonucleic Acid,ds-DNA,DNA, Double Stranded,Double-Stranded DNA,ds DNA
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
D005663 Furans Compounds with a 5-membered ring of four carbons and an oxygen. They are aromatic heterocycles. The reduced form is tetrahydrofuran. Tetrahydrofurans
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000442 Octanols Isomeric forms and derivatives of octanol (C8H17OH). Alcohols, Octyl,Heptylcarbinols,Hydroxyoctanes,Octylic Alcohols,Alcohols, Octylic,Octyl Alcohols
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
D014867 Water A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Hydrogen Oxide

Related Publications

Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
September 2017, Oncology letters,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
February 2021, Molecules (Basel, Switzerland),
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
September 2020, Bioorganic chemistry,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
March 2024, RSC medicinal chemistry,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
February 2023, RSC medicinal chemistry,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
January 2016, European journal of medicinal chemistry,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
April 2020, Future medicinal chemistry,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
January 2012, PloS one,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
January 2015, European journal of medicinal chemistry,
Yan-Cheng Wu, and Liang Cao, and Wen-Jie Mei, and Han-Qing Wu, and Shi-He Luo, and Hai-Ying Zhan, and Zhao-Yang Wang
May 2019, Bioorganic & medicinal chemistry letters,
Copied contents to your clipboard!