- Addition of lithiated 9-deazapurine derivatives to a carbohydrate cyclic imine: Convergent synthesis of the aza-C-nucleoside immucillins
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Means have been developed for the synthesis and addition of 9-deaza-9-lithiopurine derivatives to the carbohydrate-derived cyclic imine 6 in facile convergent syntheses of biologically active aza-C-nucleosides.
- Evans,Furneaux,Hutchison,Kezar,Morris, Jr.,Schramm,Tyler
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p. 5723 - 5730
(2007/10/03)
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- Substitutes O6 -benzylguanines, compositions, and methods of using same
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The present invention provides AGT inactivating compounds such as substituted O6 -benzylguanines of the formula STR1 wherein, for example, R1 is amino, hydroxy, or alkylamino, R2 is aminoalkyl, hydroxyalkyl, or alkylaminoalkyl, and R3 is halo, hydroxyalkyl, thiol or alkylthio, as well as pharmaceutical compositions comprising such compounds and 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 lesions at the O6 -position of guanine comprising administering to a mammal an effective amount of one of the aforesaid compounds and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O6 -position of guanine.
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- Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
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The present invention provides 8-substituted O6 -benzylguanines of the formula STR1 wherein R1, R2, and R3 are as defined in the specification, and 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidine, and 4(6)-substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives 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 lesions at the O6 -position of guanine, by administering to a mammal an effective amount of one of the aforesaid derivatives, 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 at the O6 -position of guanine.
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- 8-substituted O6-benzylguanine, substituted 6(4)-(benzyloxy)pyrimidine, and related derivatives as inactivators of human O6-alkylguanine-DNA alkyltransferase
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Several 8-substituted O6-benzylguanines, 2- and/or 8-substituted 6- (benzyloxy)purines, substituted 6(4)-(benzyloxy)pyrimidines, and a 6- (benzyloxy)-s-triazine were tested for their ability to inactivate the human DNA repair protein, O6/
- Chae,Swenn,Kanugula,Dolan,Pegg,Moschel
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p. 359 - 365
(2007/10/02)
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