| 摘要 |
589670 Disclosed are 2-(thiazolyl)pyrrolidine, 2-(oxazolyl)pyrrolidine and 2-(imidazolyl)pyrrolidine peptide derivatives as represented by the general formula (I), wherein: Q is alkyl, a carbocycle or a heterocycle; wherein alkyl, carbocycle and heterocycle are each optionally substituted with one or more hydroxyl, alkoxy, acyl, halogen, mercapto, oxo, carboxyl, alkyl, amino, cyano, nitro, amidino, guanidino, an optionally substituted carbocycle or an optionally substituted heterocycle; wherein one or more CH2 groups of the alkyl substituent on Q is optionally replaced with -O-, -S-, -S(O)-, S(O)2, -N(R8)-, -C(O)-, -C(O)-NR8-, -NR8-C(O)-, -SO2-NR8-, -NR8-SO2-, -NR8-C(O)-NR8-, -NR8-C(NH)-NR8-, -NR8-C(NH)-, -C(O)-O- or -O-C(O)-; X1 and X2 are each independently O or S; Y is CH2; R1 is H or R1 and R2 together form a 5-8 member ring; R2 is alkyl, a carbocycle, carbocyclylalkyl, a heterocycle or heterocyclylalkyl, each optionally substituted with halogen, hydroxyl, oxo, thione, mercapto, carboxyl, alkyl, haloallcyl, alkoxy, alkylthio, sulfonyl, amino or nitro; R3 is H or alkyl optionally substituted with halogen; or R3 and R4 together form a 3-6 member heterocycle; R3' is H or methyl, or R3 and R3' together form a 3-6 member carbocycle; R4' is H and R4 is H, alkyl, aryl, aralkyl, cycloalkyl, benzyloxycarbonyl, heteroaryl, or heterocycloalkyl, wherein said alkyl is optionally substituted with imino or heteroaryl; R5 is H or alkyl; R6 and R6' are each independently H, alkyl, aryl or aralkyl; and wherein the remaining substituents are as defined herein. Further disclosed is a pharmaceutical composition which comprises a compound as defined above and a carrier, diluent or excipient for inducing apoptosis in a cell, and for the treatment of cancer.
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