Clinical Trials with 1 , 3 - Bis ( 2 - chloroethyl ) - 1 - nitrosourea , N SC - 409962 '
نویسنده
چکیده
nitrosourea (BCNTJ) is shown in Chart 1. The back ground for the development of the nitrosoureas has been recently reviewed by Schabel et al. (4). Initial interest in the group of compounds of which BCNU is a member was stimulated by the finding of the Cancer Chemotherapy National Service Center screening program that i-methyl i-nitroso-3-nitroguanidine (NSC-9369) had weak activity against i.p. implanted Li210 leukemia. The chloroethyl and bromoethyl-substituted analogs of NSC-9369, synthe sized by Baker et al. (5), showed the most consistent ac tivity. Because of their structural relation to the nitroso guanidines, a series of nitrosoureas were synthesized and tested. The first derivative screened, i-methyl-i-ni
منابع مشابه
Clinical trials with 1,3-bis(2-chloroethyl)-1-nitrosourea, NSC-409962.
nitrosourea (BCNTJ) is shown in Chart 1. The back ground for the development of the nitrosoureas has been recently reviewed by Schabel et al. (4). Initial interest in the group of compounds of which BCNU is a member was stimulated by the finding of the Cancer Chemotherapy National Service Center screening program that i-methyl i-nitroso-3-nitroguanidine (NSC-9369) had weak activity against i.p....
متن کاملExperimental evaluation of potential anticancer agents VIII. Effects of certain nitrosoureas on intracerebral L1210 leukemia.
In quantitative therapeutic studies 1,3-bis(2-chloroethyl)-1-nitrosourea (NSC 409962) and 1-(2.-chloroethyl)-1-nitrosourea (NSC-47547) have been shown to have marked activity against intraperitoneal (I.P.) L1210 leukemia when administered by the I.P., subcutaneous, or oral route. This class of compounds is the first to be ob served to possess an encouraging degree of activity against intracereb...
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The possibility was examined that the carbamoylating activity of some chloroethylnitrosoureas could interfere with the activity of normal human cells to survive treatment with these drugs; 1-(2-chloroethyl)-3-(trans-4-hydroxycyclohexyl)-1-nitrosourea, which has strong carbamoylating activity, inhibited the rejoining of drug or X-ray-induced DNA strand breaks in IMR-90 cells, whereas the noncarb...
متن کاملEffects of Carbamoylation on Cell Survival and DMA Repair in Normal Human Embryo Cells (IMR-90) Treated with Various 1-(2-Chloroethyl)-1-nitrosoureas1
The possibility was examined that the carbamoylating activity of some chloroethylnitrosoureas could interfere with the activity of normal human cells to survive treatment with these drugs; 1-(2-chloroethyl)-3-(frans-4-hydroxycyclohexyl)-1 -nitrosourea, which has strong carbamoylating activity, inhibited the rejoining of drug or X-ray-induced DMA strand breaks in IMR-90 cells, whereas the noncar...
متن کاملMechanism of uptake of nitrosoureas by L5178Y lymphoblasts in vitro.
The mechanism of uptake of nitrosoureas by L5178Y cells in vitro was investigated. A time course of the uptake of radioactivity on incubation of L5178Y lymphoblast with [14C]-1,3-bis(2-chloroethyl)-1-nitrosourea was linear for 30 min and then entered a plateau phase; it was markedly temperature dependent. A similar time course for cells incubated with [14C]ethylene-labeled 1-(2-chlorethyl)-3-cy...
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