SPIRO DERIVATIVES OF PARTHENIN AS NOVEL ANTICANCER AGENTS

摘要

The present invention relates to novel spiro derivatives of parthenin prepared by the dipola cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nirile imide, ozone, azomethine imides, azomethine ylides etc. with exocycli double bond of C ring (a-methylene-?-butyrolactone). Representative compounds have bee screened for their anticancer activity against different cancer cell lines. ICs0 value of thes analogues varies between 4.3 µM to 93 µM. A mechanistic correlation of their anticance activity has been described. The results of the cytotoxicity test of the compounds studie indicated that the a, ß-unsaturated ketonic moity in parthenin plays an important role in th maintenance of the high level of cytotoxicity.