Title:
BENZYLGUANINE DERIVATIVE
Document Type and Number:
Japanese Patent JPH07267955
Kind Code:
A
Abstract:
PURPOSE: To obtain the subject new compound inhibiting the activity of a repair enzyme, O6-methylguanine-DNA methyltransferase, thus effective as a potentiator for alkylated carcinostatics.
CONSTITUTION: The objective derivative is expressed by formula I or formula II (X is a halogen), e.g. O6-(3-fluorobenzyl)guanine, O6-(2-fluorobenzyl)guanine. This derivative can be obtained by reaction between 2-amino-6-chloropurine and the corresponding halogenated benzyl alcohol in the presence of sodium pref. at 50-150°C for 1-10hr. Although the above two kinds of derivatives are virtually identical with each other in terms of structure, the former is dramatically highly effective in the above-mentioned inhibitory activity compared to the latter.
Inventors:
TERAJIMA ISAMU
KOYAMA KENICHI
KODA KOFUKU
MINEURA KAZUYOSHI
KOYAMA KENICHI
KODA KOFUKU
MINEURA KAZUYOSHI
Application Number:
JP8390694A
Publication Date:
October 17, 1995
Filing Date:
March 30, 1994
Export Citation:
Assignee:
TOAGOSEI CO LTD
International Classes:
C07D473/18; A61K31/52; A61K31/522; A61P35/00; A61P43/00; (IPC1-7): C07D473/18; A61K31/52