Naphthazarin derivatives (VII): Antitumor action against ICR mice bearing ascitic S-180 cells

• DOI: 10.1007/bf02976490
• Publication Date: 2008-11-03T16:33:13Z
• Authors: Gyu-Yong Song; Yong Kim; Young-Jae You; Hoon Cho; Byung-Zun Ahn
• Keywords: Male; Mice, Inbred ICR; Antineoplastic Agents; Survival Analysis; 3. Good health; Mice; Structure-Activity Relationship; Tumor Cells, Cultured; Animals; Indicators and Reagents; Drug Screening Assays, Antitumor; Sarcoma 180; Injections, Intraperitoneal; Neoplasm Transplantation; Naphthoquinones

Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydroxyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1-Hydroxyiminoalkyl)-DMNQ derivatives expressed greater antitumor action than (1-hydroxyalkyl)- or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher antitumor action than 2-sudstituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of >400%.