Isoquinoline系化合物の制癌性に関する研究(第2報) : 1-Alkyl-6,7-methylenedioxyisoquinoline誘導体の制癌性について

抄録

Based on the results previously reported, several derivatives of 1 -alkyl substituted isoquinoline were tested for antitumor activity using Ehrlich carcinoma (ascites and solid), sarcoma-180 (ascites and solid), SN-36 leukemia (ascites), and NF-sarcoma (solid) in mice. These compounds showed marked inhibitory effect on all the above tumors, although their activities were stronger in the case of ascites than in solid type. Especially marked inhibitory effects were observed with 1-(1, 1-dimethylpropyl)-3-methyl-6, 7-methylenedioxyisoquinoline·HCl (B-19), 1-(1, 1-dimethylpentyl)-6, 7-methylenedioxyisoquinoline·HCl (B-21), 1 -[(1-methylcyclopentyl)-methyl]-3-methyl-6, 7-methylenedioxyisoquinoline·HCI (B-36) and 1-[(1-methylcyc1ohexyl)methyl]-3-methyl-6, 7-methylenedioxyisoquinoline·HCl (B-36). By the effect of these compounds, number of Ehrlich ascites carcinoma cells in the ascites fluid decreased 1 hour after their administration and recovered after 24-48 hours, while the increase of degenerating cells was observed at 1-9 hours. It seemed that the antitumor activity of 1-alkyl substituted isoquinoline derivatives depended on the chemical structure of 1-alkyl residues and the actitity was greatest with tertiary or cyclo-alkyl groups.