4¼-amino podophyllotoxin congeners as potential anticancer agents and a process for the preparation thereof

摘要

The present invention provides new class of 4&bgr;-[4″-(1″,3″-benzothiazole-2″-yl)anilino]podophyllotoxin analogues having the structural formula as follows (4). Where R═H or CH3; R1═H, halogen, CH3 and R2═H, halogen, OCH3. The present invention also provides a process for the preparation of new 4&bgr;-[4″-(1″, 3″-benzothiazole-2″-yl)anilino]podophyllotoxin analogues as useful anticancer agents. More particularly, it provides a process for the preparation of 4&bgr;-[4″-(1″,3″-benzothiazole-2″-yl)anilino] derivatives of podophyllotoxin. The process for the synthesis of new podophyllotoxin analogues as anticancer agents produces the novel and stereo-selective derivatives of the podophyllotoxin in good yields, where in the key step for the synthesis of these analogues is by direct nucleophilic substitution of C-4&bgr;-iodo intermediates. The 4&bgr;-iodopodophyllotoxin, which has been reacted with substituted or unsubstituted 4-(1,3-benzothiazole-2-yl)aniline in a stereo-selective manner to afford the 4&bgr;-[4″-(1″,3″-benzothiazole-2″-yl)anilino] derivatives of podophyllotoxin.