title: Synthesis and anticancer activity of some novel 2-phenazinamine derivatives.
abstract: 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.
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Xiaochun
authors.initials: X
authors.lastname: Gao
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Lu
authors.forename: Lei
authors.initials: L
authors.lastname: Fang
authors.forename: Xubin
authors.initials: X
authors.lastname: Fang
authors.forename: Yingying
authors.initials: Y
authors.lastname: Xing
authors.forename: Shaohua
authors.initials: S
authors.lastname: Gou
authors.forename: Tao
authors.initials: T
authors.lastname: Xi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D057809:HEK293 Cells; D056945:Hep G2 Cells; D006801:Humans; D020014:K562 Cells; D061986:MCF-7 Cells; D015394:Molecular Structure; D010619:Phenazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D010619:Phenazines
keywords: 2-Phenazinamine derivatives; Anticancer activity; Apoptosis; MTT assay