Synthesis and anticancer activity of 5,6,8,13-tetrahydro-7H-naphtho[2,3-a][3]-benzazepine-8,13-diones.

Abstract

A series of naphthoquinones fused benzazepines, 5,6,8,13-tetrahydro-7H-naphtho[2,3-a][3]-benzazepine-8,13-diones, were synthesized and evaluated for their anticancer activity against four cell lines; human breast carcinoma cell line, human cervix carcinoma cell line, human hepatocellular carcinoma cell line and human keratinocyte cell line. The results showed that 5,6,8,13-tetrahydro-2,3,4,9-tetramethoxy-7H-naphtho[2,3-a][3]benzazepine-8,13-dione 4g and 5,6,8,13-tetrahydro-2,3,9-trimethoxy-7H-naphtho[2,3-a][3]benzazepine-8,13-dione 4h have significant cytotoxicity against a hepatocellular carcinoma cell line with IC(50) = 3.5 μg/mL and 3.0 μg/mL, respectively.

• Authors: Weerachai Phutdhawong, Gedsirin Eksinitkun, Wanwikar Ruensumran, Thongchai Taechowisan, Waya S Phutdhawong
• Journal: Archives of pharmacal research (Arch Pharm Res) Vol. 35 Issue 5 Pg. 769-77 (May 2012) ISSN: 1976-3786 [Electronic] Korea (South)
• PMID: 22644844 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Naphthoquinones

Topics

• Cell Line
• Cell Line, Tumor
• Drug Evaluation, Preclinical
• HeLa Cells
• Hep G2 Cells
• Humans
• Keratinocytes (drug effects, physiology)
• Naphthoquinones (chemical synthesis, pharmacology)