Abstract
The spin labeled derivatives of podophyllotoxin, 4-[4″−(2″, 2″, 6″, 6″-tetramethyl-1″-piperidinyloxy)amino] −4′-demethylepipodophyllotoxin(GP-7, 3 ) and N-podophyllic acid-N″-[4-(2,2,6,6,-tetramethyl-1-piperidinyloxy)] thiosemicarbazide (GP-4, 5 ) were synthesized and tested for their anticancer activity against the mouse solid tumors S180 and HepA in vivo , and the mouse lymphocytic leukemia L1210 and human stomach carcinoma SGC-7901 cells in vitro . At equitoxic concentrations, the anticancer activity of GP-7( 3 ) was found to be similar to that of the clinically used VP-16( 2 ). The toxicity of GP-7( 3 ) (LD 50231.2 mg/Kg) is 3.3 times lower than that of VP-16 (LD 50 69.5 mg/Kg). GP-7(3) exhibits low subchronic toxicity. The total chemical yield of GP-7 (26%) is 4 times higher than that of VP-16 (6%) (based on podophyllotoxin). Therefore, GP-7( 3 ) seems to be a promising new entry into the podophyllotoxin class of anticancer drugs.
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