摘要 |
The present invention provides AGT inactivating compounds such as substituted O6-benzylguanines of formula (I) wherein 7- or 9-substituted 8-aza-O6- benzylguanines, 7,8-disubstituted O6-benzylguanines, 7,9-disubstituted O6-benzylguanines, 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidines, and 4(6)--substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidines, as well as pharmaceutical compositions comprising such compounds along with a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesion at the O6-position of guanine, by administerin g to a mammal an effective amount of one of the aforesaid compounds, 2,4-diamino-6-benzyloxy-s-triazine, 5-substituted 2,4-diamino-6- benzyloxypyrimidines, or 8-aza-O6-benzylguanine, and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions of the O6-position of guanine.
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申请人 |
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY OF THE DEP ART;ARCH DEVELOPMENT CORPORATION, THE UNIVERSITY OF CHICAGO THE UNIVERSITY OF CH;THE PENN STATE RESEARCH FOUNDATION |
发明人 |
MOSCHEL, ROBERT C.;PEGG, ANTHONY E.;DOLAN, M. EILEEN;CHAE, MI-YOUNG |