Journal of Organic Chemistry p. 2749 - 2753 (1987)
Update date:2022-09-26
Topics:
Glinski, Margaret B.
Freed, James C.
Durst, Tony
A series of 2-substituted podophyllotoxin derivatives, including 2-methyl-, 2-chloro-, 2-hydroxy-, and 2-bromopodophyllotoxin, were prepared, in order to determine whether nonenolizable podophyllotoxins had enhanced in vivo activity against P388 and L1210 tumor cells.Significant activity against P388 (T/C 156, 40 mg/kg) was observed for 2-chloropodophyllotoxin; under similar conditions, podophyllotoxin was toxic.The corresponding 2-picro isomers were formed as byproducts in the above reactions and were, when tested, inactive against tumors at similar concentrations.An attempt to prepare 2-fluoropodophyllotoxin by reacting podophyllotoxin 4-O-THP enolate with FClO3 resulted in a violent explosion, causing serious injury.Extreme caution should be taken when reacting enolates with FClO3.
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