SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-β-ALKOXYLCARBONYL-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN

AIM　To search for more potential and lower toxicity antitumor drugs. METHODS AND RESULTS　Thirty eight new 4-β-ester substituted-4-deoxy-4′-demethylepipodophylotoxin derivatives(II-1～II-38) were designed and synthesized. All compounds were screened in vitro against L1210 leukemia and KB cells. CONCLUSION　Fatty esters showed higher activity than aromatic esters. II-10 exhibited the highest activity, which is more than 100-fold of etoposide. For fatty esters, the compounds with less than 3 carbons in the main chain have higher activity, while for aromatic esters, those having electron-attracting substituents in the aromatic ring are more active.