Isoquinoline系化合物の制癌性に関する研究(第1報) : HeLaおよびEhrlichに対する活性と構造相関について

抄録

Relationship between chemical constitution and antitumor activity of isoquinoline derivatives was examined, and the following results were obtained. These compounds were classified into five types according to the substituent at 1-position of the isoquinoline ring, and their in vitro activity against HeLa cells and in vivo activity against Ehrlich ascites carcinoma were tested. A parallelism was found between the in vitro and in vivo activities and the alkyl type compounds, especially the ones possessing tertiaryalkyl or cycloalkyl group in 1-position showed a marked inhibitory effect, while the other four types were only slightly active. These data suggested that the antitumor activity of isoquinoline derivatives was mainly determined by the chemical structure of the substituent at 1-position and in the alkyl type compounds the activity increased as the number of carbon atoms in the alkyl increased.