Synthesis and Biological Activity of Novel Spin Labeled Derivatives of 4＇-Demethyl-4-deoxypodophyllotoxin

Seven novel spin labeled derivatives of 4＇-demethyl-4-deoxypodophyllotoxin with nitroxyl radi- cals（TMHPO and TMPRO） were prepared and their cytotoxic and antioxidative activities were tested. Their cytotoxic activities were tested against two tumor cell lines（A-549 and HL-60） in vitro. Among them, five compounds show higher inhibition activity against A-549 cells compared with the clinical drug VP-16（2） and parent compound 4＇-demethyl-4-deoxypodophyllotoxin（DDPT, 6）. Compounds 8, 10 and 13 show excellent inhibition activity against HL-60 cells. Furthermore, the antioxidative activities of them were tested. All the seven spin labeled compounds show stronger antioxidative activity compared with VP-16（2） and DDPT（6）. The partition coefficients P of these derivatives were determined.