Antitumor activity of 13-methyl-berberrubine derivatives

Abstract

The antitumor activity of several 13-alkyl-berberrubine and newly synthesized ester derivatives, using experimental tumors (S-180, NF sarcoma, Ehrlich carcinoma and L-1210) in mice was tested. For chemotherapeutic evaluation, the therapeutic indices and ratios were determined. Our present findings confirmed that in berberrubine derivatives, the 9-demethyl structure was essential for the manifestation of antitumor activity and demonstrated that ester derivatives also exhibit a remarkable antitumor activity, and the 13-methyl derivatives of both berberrubine and palmatrubine alkaloids showed high antitumor activity. © 1982, The Pharmaceutical Society of Japan. All rights reserved.