Synthesis and anticancer activity of some novel 2-phenazinamine derivatives

• A novel series of 2-phenazinamine derivatives were synthesized and spectrally characterized.
• Several compounds exhibited potent anticancer activity.
• Compound 4 showed more potency against HepG2 cell lines than the positive control cisplatin in terms of IC50 values.
• Compound 4 significantly induced apoptosis of HepG2 cancer cells.

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.

A novel series of 2-phenazin-amine derivatives were synthesized based on the natural product, N-(2-hydroxyphenyl)-2-phenazinamine and spectrally characterized. Compound 4 exhibited more potency against HepG2 cell line than the positive control cisplatin in terms of IC50 values.Figure optionsDownload as PowerPoint slide