BIOMAT Database Logo BIOMAT Database Logo

Discovery and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro. 2017

Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Jiangsu Key Laboratory of Drug Design and Optimization, School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, China.

Phenotypic screening of high quality compound library is one of the most effective strategy to obtain novel bioactive compounds. Recently, our group have constructed a Wogonin-scaffold library with substituents diversity and successfully obtained a series of potent compounds. Herein, we reported the synthesis of these compounds and evaluated the in vitro antitumor activity against a panel of human tumor cell lines. Most of them showed good activity with a broad spectrum and preliminary structure-activity relationship for the substitutions were obtained. Further biological assays showed that the most potent compounds 18n and 20b could significantly enhance the intracellular ROS level and induce the cell apoptosis at low micromole level. Through similarity searching, CDK9 was identified as the potential target for 20b, which could be a start point for next structure-based drug design.

UI MeSH Term Description Entries
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
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
D017209 Apoptosis A regulated cell death mechanism characterized by distinctive morphologic changes in the nucleus and cytoplasm, including the endonucleolytic cleavage of genomic DNA, at regularly spaced, internucleosomal sites, i.e., DNA FRAGMENTATION. It is genetically programmed and serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth. Apoptosis, Extrinsic Pathway,Apoptosis, Intrinsic Pathway,Caspase-Dependent Apoptosis,Classic Apoptosis,Classical Apoptosis,Programmed Cell Death,Programmed Cell Death, Type I,Apoptoses, Extrinsic Pathway,Apoptoses, Intrinsic Pathway,Apoptosis, Caspase-Dependent,Apoptosis, Classic,Apoptosis, Classical,Caspase Dependent Apoptosis,Cell Death, Programmed,Classic Apoptoses,Extrinsic Pathway Apoptoses,Extrinsic Pathway Apoptosis,Intrinsic Pathway Apoptoses,Intrinsic Pathway Apoptosis
D017382 Reactive Oxygen Species Molecules or ions formed by the incomplete one-electron reduction of oxygen. These reactive oxygen intermediates include SINGLET OXYGEN; SUPEROXIDES; PEROXIDES; HYDROXYL RADICAL; and HYPOCHLOROUS ACID. They contribute to the microbicidal activity of PHAGOCYTES, regulation of SIGNAL TRANSDUCTION and GENE EXPRESSION, and the oxidative damage to NUCLEIC ACIDS; PROTEINS; and LIPIDS. Active Oxygen Species,Oxygen Radical,Oxygen Radicals,Pro-Oxidant,Reactive Oxygen Intermediates,Active Oxygen,Oxygen Species, Reactive,Pro-Oxidants,Oxygen, Active,Pro Oxidant,Pro Oxidants,Radical, Oxygen
D044950 Flavanones A group of FLAVONOIDS characterized with a 4-ketone. 2-Phenyl-Benzopyran-4-Ones,2 Phenyl Benzopyran 4 Ones
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
D055808 Drug Discovery The process of finding chemicals for potential therapeutic use. Drug Prospecting,Discovery, Drug,Prospecting, Drug
D066244 Proton Magnetic Resonance Spectroscopy Spectroscopy technique which measures changes in organic compounds by tracking the spectral energy of absorption of HYDROGEN atoms. 1H NMR,1H-MRS,1H-NMR

Related Publications

Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Discovery of novel bis-evodiamine derivatives with potent antitumor activity.
July 2022, Bioorganic & medicinal chemistry,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Discovery of pyrazolone spirocyclohexadienone derivatives with potent antitumor activity.
January 2020, Bioorganic & medicinal chemistry letters,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Synthesis and antitumor activity in vitro of novel berbamine derivatives.
July 2021, Journal of Asian natural products research,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Synthesis and in vitro antitumor activity of novel scopoletin derivatives.
August 2012, Bioorganic & medicinal chemistry letters,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Discovery of Novel Quinazoline Derivatives as Potent Antitumor Agents.
June 2022, Molecules (Basel, Switzerland),
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity.
March 2019, European journal of medicinal chemistry,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
June 2011, European journal of medicinal chemistry,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
September 2001, Journal of medicinal chemistry,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
January 2019, Journal of medicinal chemistry,
Jubo Wang, and Raoling Ge, and Xiaqiu Qiu, and Xi Xu, and Libin Wei, and Zhiyu Li, and Jinlei Bian
Discovery of Novel 8-Hydroxyquinoline Derivatives with Potent In Vitro and In Vivo Antifungal Activity.
December 2023, Journal of medicinal chemistry,
Copied contents to your clipboard!