| 摘要 |
Disclosed are heteroaryl oligopeptide derivatives as represented by the general formula (I), wherein wherein Ra, Rb and Rc are each independently hydroxyl, halogen, alkyl, alkoxy, alkylthio or sulfonyl; or two of Ra, Rb and Rc together form a carbocycle or heterocycle and the other of Ra, Rb and Rc is H, hydroxyl, halogen, alkyl, alkoxy, alkylthio or sulfonyl; or Ra is H while Rbb and Rc are each independently hydroxyl, halogen, alkyl, alkoxy, alkylthio or sulfonyl; or two of Ra, Rb and Rc together form a carbocycle or heterocycle and the other of Ra, Rb and Rc is H, hydroxyl, halogen, alkyl, alkoxy, alkylthio or sulfonyl; X1, X2 and X3 are each independently O or S; R1 is H or alkyl; R2 is alkyl, a carbocycle, carbocyclylalkyl, a heterocycle or heterocyclylalkyl, each of which may be optionally substituted; R3 is H or alkyl optionally substituted with halogen or hydroxyl; or R3 and R4 together form a 3-6 membered heterocycle; R4 and R4' are independently H, hydroxyl, amino, alkyl, carbocycle, carbocycloalkyl, carbocycloalkyloxy, carbocycloalkyloxycarbonyl, heterocycle, heterocycloalkyl, heterocycloalkyloxy or heterocycloalkyloxycarbonyl; or R4 and R4' together form a heterocycle; R5 is H or alkyl; G is -C(=X3)NR5''-A1; wherein R5' is H or alkyl; and A1 is an optionally substitued 5-member heterocycle comprising 1 to 4 heteroatoms; and salts and solvates thereof. Further disclosed is a pharmaceutical composition which comprises a compound as defined above and a therapeutically inert carrier, diluent or excipient, for treating a disease or condition associated with the overexpression of an lAP in a mammal, and particularly for treating cancer.
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