主权项 |
1. A conjugate comprising:
at least one modified amino acid residue of the formula: wherein X is N, NH, O, S, CH or CH2; Y1 and Y2 are each independently selected from N, O and S; n is 1 or 2; R2 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl; R3 is selected from alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl amino, alkylamide, substituted alkylamide, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl; R4 is optional and if present is selected from hydrogen, hydroxyl, halogen, cyano, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkylalkoxy, substituted alkylalkoxy, acyl, carboxyl, and carboxyl ester; R5 is optional and if present is hydrogen or hydroxyl; and R6 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl amino, alkylamide, substituted alkylamide, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl, wherein one of W1 and W2 is a polypeptide and the other is a drug or a detectable label, wherein the dotted lines represent optional bonds, wherein when the dotted line between the R4-carbon and the R5-carbon is a double bond, n is 1 and R4 and R5 are not present, and wherein, when n is 2, the dotted line between the R4-carbon and the R5-carbon is not a double bond and R5 is not present. |