Naphthazarin derivatives (VII): antitumor action against ICR mice bearing ascitic S-180 cells.
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%.
Song
G Y
GY
College of Pharmacy, Chungnam National University, Taejon, Korea.
Kim
Y
Y
You
Y J
YJ
Cho
H
H
Ahn
B Z
BZ
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009285:Naphthoquinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D009368:Neoplasm Transplantation; D012510:Sarcoma 180 / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D016019:Survival Analysis
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D009285:Naphthoquinones; C005503:naphthazarin