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.
