| abstract |
Compounds having particular interest as labels and various novel uses in diagnostics and therapeutics are provided which have structure (1) n n n wherein R 1 is a binding partner, a linker or H; n a and b are 0 or 1, provided that the total of a and b is 0 or 1; n A is N or C; n X is S, O, —C(O)—, NH or NCH 2 R 6 ; n Y is —C(O)—; n Z is taken together with A to form an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O and a single N ring heteroatom separated by a carbon atom, a single S and a single N ring heteroatom separated by a carbon atom, 2 N ring heteroatoms separated by a carbon atom, or 3 N ring heteroatoms at least two of which are separated by a carbon atom, and wherein the aryl or heteroaryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R 6 or ═O; n R 6 is independently H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, NO 2 , N(R 3 ) 2 , C≡N or halo, or an R 6 is taken together with an adjacent R 6 to complete a ring containing 5 or 6 ring atoms; n R 3 is a protecting group or H; and tautomers, solvates and salts thereof; and provided that where a is 0, b is 1, and R 1 is n n n in which D 2 is independently hydroxyl, blocked hydroxyl, mono, di or triphosphate, or an oligodeoxyribonucleotide otherwise containing only the bases A, G, T and C; and n D 3 is H or OH; n then Z is not unsubstituted phenyl. n Also provided are novel intermediates and methods for the preparation and use of the structure (1) compounds. |