An efficient one-pot synthesis of benzothiazolo-4β-anilino-podophyllotoxin congeners: DNA topoisomerase-II inhibition and anticancer activity

A facile one-pot zirconium tetrachloride and sodium iodide mediated iodination protocol has been applied for the synthesis of benzothiazolo-4β-anilino-podophyllotoxin (5a-h) and benzothiazolo-4β-anilino-4-O-demethylepipodophyllotoxin (6a-h) congeners. Some of these compounds have shown significant in vitro cytotoxicity on selected human cancer cell lines apart from DNA topoisomerase-II inhibition activity.