Journal of Medicinal Chemistry p. 1667 - 1675 (1990)
Update date:2022-07-29
Topics:
Anderson, Wayne K.
Dean, Dennis C.
Endo, Toshiyasu
A series of 4- and 5-<2,3-dihydro-6,7-bis<<(N-alkylcarbamoyl)oxy>methyl>-1H-pyrrolizin-5-yl>-2-halopyridinium iodides were synthesized.The rates of hydrolysis of the α-halopyridinium salts to the corresponding pyridones, and the reactivities of the carbamate moieties were studied as a function of pH, buffer composition, and ionic strength.The 4- and 5-pyrrolizinyl-2-halopyridinium iodides and the corresponding pyridones were evaluated against P388 lymphocytic leukemia in vivo.The α-fluoropyridinium compounds were active but the α-chloro compounds were not.This activity was correlated with the rates of hydrolysis of the α-halopyridinium compounds to the active pyridone.Compounds that were active in the P388 screen were evaluated in L1210 leukemia, M5076 carcinoma, and MX-1 mammary xenograft assays in mice.
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