ANTITUMOR ACTIVITY OF 5-SUBSTITUTED 3-(1'-ANILINOETHYLIDENE) PYRROLIDINE-2, 4-DIONE

Antitumor activity of various compounds of tenuazonic acid analogs, 5-substituted 3-(1'-anilinoethylidene)pyrrolidine-2, 4-dione, was tested in vitro and in vivo. Among these compounds, 5-benzyl and 5-(p-hydroxybenzyl) derivatives were found to be highly effective against Yoshida sarcoma cells in vitro and Ehrlich ascites tumor in vivo. The latter compound was also active against Yoshida sarcoma and L-1210 in vivo. The optical activity of the active compound does not seem to concern the antitumor activity. Structure-activity relationship of these compounds was discussed.