| 摘要 |
The invention provides alpha -mimetic structure of formula (I) wherein A is -(C=O)-CHR3-, or -(C=O), B is N-R3- or -CHR6-, D is -(C=O)-(CHR7)- or - (C=O) E is -(ZR8)- or (C=O), G is -(XR9)n-, -(CHR10)-(NR6)-, -(C=O)-(XR12)-, -(C=N-W-R1)-, -(C=O)-, X-(C=O)-R13, X-(C=O)-NR13R14, X-(SO2)-R13, or X-(C=O)-OR13, W is -Y(C=O)-, -(C=O)NH-, -(SO2)-, -CHR14, (C=O)-(NR15)-, substituted or unsubstituted oxadiazole, substituted or unsubstituted triazole, substituted or unsubstituted thiadiazole, substituted or unsubstituted 4,5 dihydrooxazole, substituted or unsubstituted 4,5 dihydrothiazole, substituted or unsubstituted 4,5 dihydroimidazole, or nothing, Y is oxygen or sulfur, X and Z is independently nitrogen or CH, n=0 or 1; and R1 R2, R3, R4, R5, R6, R7, R8, R9 R10, R11, R12, R13, R14, and R15 are the same or different and independently selected from an amino acid side chain moiety or derivative thereof, the remainder of the molecule, a linker and a solid support, and stereoisomers, salts, and prodrugs thereof, provided that where B is CHR6 and W is -Y(C=O)-, -(C=O)NH-, -(SO2), -CHR14, or (C=O)-(NR15)-, G cannot be CHR9, NR9, (C=O)-CHR12, (C=O)-NR12, or no atom at all. Additionally, the invention provides methods wherein .alpha.-mimetic compounds are used to treat cancer stem cells . |
