160948-35-6Relevant academic research and scientific papers
6,5-HETEROCYCLIC PROPARGYLIC ALCOHOL COMPOUNDS AND USES THEREFOR
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Page/Page column 80, (2015/05/06)
The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
Substitutes O6 -benzylguanines, compositions, and methods of using same
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, (2008/06/13)
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.
Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
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, (2008/06/13)
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.
8-substituted O6-benzylguanine, substituted 6(4)-(benzyloxy)pyrimidine, and related derivatives as inactivators of human O6-alkylguanine-DNA alkyltransferase
Chae,Swenn,Kanugula,Dolan,Pegg,Moschel
, p. 359 - 365 (2007/10/02)
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/
Structure-Activity Relations. Part 12. Antibacterial Activity of a Series of 2,4-Diamino-6-substituted 5-(4-pyridylmethylamino)pyrimidines and 2,4-Diamino-5-(4-substituted benzylamino)pyrimidines.
Bowden, Keith,Bright, Andrew C.
, p. 514 - 539 (2007/10/02)
A series of 6-substituted 2,4-diamino-5-(4-pyridylamino)pyrimidines and of 2,4-diamino-5-(4-substituted benzylamino)pyrimidines has been prepared.Their antibacterial activity towards L. casei, S. aureus and E. coli has been investigated.These activities have been successfully correlated by Hansch-type relations.Dependence on both lipophilicity and electronic (polar) factors has been found.The results are related to the structure and interactions with the receptor.
