BIOMAT Database Logo BIOMAT Database Logo

Synthesis and anticancer activity of some novel 2-phenazinamine derivatives. 2013

Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.

In this study, we report the synthesis and spectral characterization of a novel series of 2-phenazinamine derivatives. In vitro evaluation for their anticancer activity toward cultured K562 (human chronic myelogenous leukemia), HepG2 (human hepatocellular carcinoma), MGC803 (human gastric carcinoma), HCT116 (human colorectal carcinoma), MCF7 (human breast adenocarcinoma) cell lines, as well as 293T (epithelial cells from human embryo kidney) non-cancer cell was carried out. The compounds 4, 7, 16 and 19 showed good positive anticancer activity in vitro. In particular, compound 4, 2-chloro-N-(phenazin-2-yl)benzamide, possessed a potent anticancer effect comparable to cisplatin against both K562 and HepG2 cancer cells but was very low or had no effect against 293T non-cancer cell. Preliminary anticancer mechanism of 4 was investigated by cell apoptosis assays compared with cisplatin using flow cytometry.

UI MeSH Term Description Entries
D010619 Phenazines
D002470 Cell Survival The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability. Cell Viability,Cell Viabilities,Survival, Cell,Viabilities, Cell,Viability, Cell
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
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
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
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
D045325 HCT116 Cells Human COLORECTAL CARCINOMA cell line. HCT 116 Cells,HCT-116 Cells,Cell, HCT 116,Cell, HCT-116,Cell, HCT116,Cells, HCT 116,Cells, HCT-116,Cells, HCT116,HCT 116 Cell,HCT-116 Cell,HCT116 Cell

Related Publications

Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Synthesis and anticancer activity of some novel 2-substituted benzimidazole derivatives.
July 2010, European journal of medicinal chemistry,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Synthesis, anti-inflammatory and anticancer activity evaluation of some novel acridine derivatives.
February 2010, European journal of medicinal chemistry,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Anticancer agents. II. Synthesis and antimycobacterial activity of some novel methylglyoxal derivatives.
January 1967, Proceedings of the Royal Irish Academy. Section B: Biological, geological, and chemical science,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Synthesis, anticancer activity and radiosensitizing evaluation of some new 2-pyridone derivatives.
March 2012, Arzneimittel-Forschung,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Synthesis and evaluation of in vitro anticancer activity of some novel isopentenyladenosine derivatives.
June 2010, Bioorganic & medicinal chemistry,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Novel myricetin derivatives: Design, synthesis and anticancer activity.
June 2015, European journal of medicinal chemistry,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Novel N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives: Synthesis and anticancer activity evaluation.
November 2020, Bioorganic chemistry,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Synthesis, anticancer and radiosensitizing evaluation of some novel sulfonamide derivatives.
March 2015, European journal of medicinal chemistry,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Design, synthesis and anticancer activity evaluation of some novel pyrrolo[1,2-a]azepine derivatives.
July 2014, Archiv der Pharmazie,
Xiaochun Gao, and Yuanyuan Lu, and Lei Fang, and Xubin Fang, and Yingying Xing, and Shaohua Gou, and Tao Xi
Synthesis and anticancer activity of some novel tetralin-6-yl-pyrazoline, 2-thioxopyrimidine, 2-oxopyridine, 2-thioxo-pyridine and 2-iminopyridine derivatives.
April 2011, Molecules (Basel, Switzerland),
Copied contents to your clipboard!