Compounds and therapeutic use thereof for protein kinase inhibition

摘要

Novel compound having the following formula: (I) wherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.;

主权项

1. A compound of formula I:wherein
Y═NH, R1=selected from following groups:wherein X═CH2, NH, S, or O,
R8═—H, —NH2, —OH, —N(R4, R5), —C(R4R5)1-7NR6R7, —C(R4R5)1-7OR6, or —N(R4)NR5R6, wherein R4, R5, R6, R7═H, alkyls (C1-C6), cycloalkyls (C3-C8) with or without nuclear heteroatoms selected from the group consisting of O, S, and N, aryls (either unsubstituted or substituted), or heteroaromatics (either unsubstituted or substituted), R9, R10, R11, R12, and R13═H, alkyls (C1-C6), cycloalkyls (C3-C8) with or without nuclear heteroatoms selected from the group consisting of O, S or N; aryls (either unsubstituted and substituted), or heteroaromatics (either unsubstituted or substituted), R2 is selected from a group consisting of H, OH, NH2, OR14, NR14R15, alkyl, aryl, heteroaryl, cycloalkyl, arylalkyl, heterocyclyl, heterocyclylalkyl, alkenyl, and alkynyl, wherein R14, R15═H, alkyls (C1-C6), cycloalkyls (C3-C8) with or without nuclear heteroatoms selected from the group consisting of O, S, N, aryls (either unsubstituted or substituted), or heteroaromatics (either unsubstituted or substituted), and R3 is selected from a group consisting of H, alkyl, aryl, heteroaryl, cycloalkyl, arylalkyl, heterocyclyl, heterocyclylalkyl, alkenyl, and alkynyl.