Inhibitors of Checkpoint Kinases

1 . A compound of the Formula A:

wherein:

X 1 , X 2 , X 3 and X 4 are independently selected from CH and N;

a is 0 or 1; b is 0 or 1; m is 0, 1, or 2; n is 1, 2, 3 or 4; p is 1 or 2; q is 1 or 2;

Ring Z is selected from: aryl, heteroaryl, heterocyclyl and (C 4 -C 8 )cycloalkyl;

R 1 is selected from: H, (C═O) a O b C 1 -C 10 alkyl, (C═O) a O b aryl, (C═O) a O b C 2 -C 10 alkenyl, (C═O) a O b C 2 -C 10 alkynyl, CO 2 H, halo, OH, O b C 1 -C 6 perfluoroalkyl, (C═O) a NR 7 R 8 , CN, (C═O) a O b C 3 -C 8 cycloalkyl, S(O) m NR 7 R 8 , S(O) m —(C 1 -C 10 )alkyl, SH and (C═O) a O b heterocyclyl, said alkyl, aryl, alkenyl, alkynyl, cycloalkyl, and heterocyclyl is optionally substituted with one or more substituents selected from R 6 ;

R 2 is selected from: H, (C═O) a O b C 1 -C 10 alkyl, (C═O) a O b aryl, (C═O) a O b C 2 -C 10 alkenyl, (C═O) a O b C 2 -C 10 alkynyl, CO 2 H, Br, I, OH, O b C 1 -C 6 perfluoroalkyl, (C═O) a NR 7 R 8 , CN, (C═O) a O b C 3 -C 8 cycloalkyl, S(O) m NR 7 R 8 , S(O) m —(C 1 -C 10 )alkyl, SH and (C═O) a O b heterocyclyl, said alkyl, aryl, alkenyl, alkynyl, cycloalkyl, and heterocyclyl is optionally substituted with one or more substituents selected from R 6 ;

R 3 is selected from: H, (C═O) a O b C 1 -C 10 alkyl, (C═O) a O b aryl, (C═O) a O b C 2 -C 10 alkenyl, (C═O) a O b C 2 -C 10 alkynyl, CO 2 H, Br, I, OH, O b C 1 -C 6 perfluoroalkyl, (C═O) a NR 7 R 8 , CN, (C═O) a O b C 3 -C 8 cycloalkyl, S(O) m NR 7 R 8 , S(O) m —(C 1 -C 10 )alkyl, SH and (C═O) a O b heterocyclyl, said alkyl, aryl, alkenyl, alkynyl, cycloalkyl, and heterocyclyl is optionally substituted with one or more substituents selected from R 6 ;

R 6 is: (C═O) a O b C 1 -C 10 alkyl, (C═O) a O b aryl, C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, (C═O) a O b heterocyclyl, CO 2 H, halo, CN, OH, O b C 1 -C 6 perfluoroalkyl, O a (C═O) b NR 7 R 8 , oxo, CHO, (N═O)R 7 R 8 , S(O) m NR 7 R 8 , S(O) m —(C 1 -C 10 )alkyl, SH or (C═O) a O b C 3 -C 8 cycloalkyl, said alkyl, aryl, alkenyl, alkynyl, heterocyclyl, and cycloalkyl optionally substituted with one or more substituents selected from R 6a ;

R 6a is selected from: (C═O) a O b (C 1 -C 10 )alkyl, O a (C 1 -C 3 )perfluoroalkyl, (C 0 -C 6 )alkylene-S(O) m R a , oxo, OH, halo, CN, (C 2 -C 10 )alkenyl, (C 2 -C 10 )alkynyl, (C 3 -C 6 )cycloalkyl, (C 0 -C 6 )alkylene-aryl, (C 0 -C 6 )alkylene-heterocyclyl, (C 0 -C 6 )alkylene-N(R b ) 2 , C(O)R a , (C 0 -C 6 )alkylene-CO 2 R a , C(O)H, and (C 0 -C 6 )alkylene-CO 2 H, said alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heterocyclyl is optionally substituted with up to three substituents selected from R b , OH, (C 1 -C 6 )alkoxy, halogen, CO 2 H, CN, O(C═O)C 1 -C 6 alkyl, oxo, and N(R b ) 2 ;

R 7 and R 8 are independently selected from: H, (C═O)O b C 1 -C 10 alkyl, (C═O)O b C 3 -C 8 cycloalkyl, (C═O)O b aryl, (C═O)O b heterocyclyl, C 1 -C 10 alkyl, aryl, C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, heterocyclyl, C 3 -C 8 cycloalkyl, S(O) m R a , and (C═O)NR b 2 , said alkyl, cycloalkyl, aryl, heterocylyl, alkenyl, and alkynyl is optionally substituted with one or more substituents selected from R 6a , or R 7 and R 8 can be taken together with the nitrogen to which they are attached to form a monocyclic or bicyclic heterocycle with 3-7 members in each ring and optionally containing, in addition to the nitrogen, one or two additional heteroatoms selected from N, O and S, said monocylcic or bicyclic heterocycle optionally substituted with one or more substituents selected from R 6a ;

R a is H, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, aryl, or heterocyclyl; and

R b is independently H, (C 1 -C 6 )alkyl, aryl, heterocyclyl, (C 3 -C 6 )cycloalkyl, (C═O)OC 1 -C 6 alkyl, (C═O)C 1 -C 6 alkyl or S(O) m R a ;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

2 . The compound according to claim 1 of the Formula B:

wherein:

all other substituents and variables are as defined in claim 1 ;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

3 . The compound according to claim 1 of the Formula C:

wherein:

all other substituents and variables are as defined in claim 1 ;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

4 . The compound according to claim 1 of the Formula D:

wherein:

all other substituents and variables are as defined in claim 1 ;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

5 . The compound according to claim 1 of the Formula E:

wherein:

all other substituents and variables are as defined in claim 1 ;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

6 . The compound according to claim 1 of the Formula F:

wherein:

all other substituents and variables are as defined in claim 1 ;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

7 . A compound according to claim 1 which is selected from:

9-chlorobenzo[h]isoquinolin-1(2H)-one;

4-bromo-9-chlorobenzo[h]isoquinolin-1(2H)-one;

9-chloro-4-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

9-chloro-4-phenylbenzo[h]isoquinolin-1(2H)-one;

9-chloro-4-[4-(hydroxymethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

9-chloro-4-[3-(hydroxymethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

9-chloro-4-(1H-pyrazol-3-yl)benzo[h]isoquinolin-1(2H)-one;

9-chloro-4-vinylbenzo[h]isoquinolin-1(2H)-one;

4-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)benzoic acid;

3-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)benzoic acid;

9-chloro-4-[(E)-2-phenylvinyl]benzo[h]isoquinolin-1(2H)-one;

4-{[4-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)phenyl]amino}-4-oxobutanoic acid;

3-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)benzonitrile;

N-[3-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)phenyl]acetamide;

9-chloro-4-(1-methyl-1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

9-chloro-4-cyclohex-1-en-1-ylbenzo[h]isoquinolin-1(2H)-one;

3-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)benzamide;

3-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)-N-[2-(dimethylamino)ethyl]benzamide;

9-chloro-4-{3-[(4-methylpiperazin-1-yl)carbonyl]phenyl}benzo[h]isoquinolin-1(2H)-one;

4-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)-N-[2-(dimethylamino)ethyl]benzamide;

4-{[3-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-4-yl)phenyl]amino}-4-oxobutanoic acid;

9-chloro-4-(6-oxo-1,6-dihydropyridin-3-yl)benzo[h]isoquinolin-1(2H)-one;

9-chloro-4-pyridin-3-ylbenzo[h]isoquinolin-1(2H)-one;

9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carbonitrile;

9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-(1H-pyrazol-4-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carbonitrile;

1-oxo-9-(2-thienyl)-1,2-dihydrobenzo[h]isoquinoline-6-carbonitrile;

1-oxo-9-(1H-pyrrol-2-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carbonitrile;

1-oxo-9-(1H-pyrazol-4-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carbonitrile;

methyl 1-oxo-9-(1H-pyrrol-2-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-phenyl-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(4-hydroxy phenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-thien-3-yl-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(1-methyl-1H-pyrazol-4-yl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

4-[6-(methoxycarbonyl)-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl]pyridine;

methyl 9-[4-(aminomethyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[3-(hydroxymethyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[4-(hydroxymethyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-(1H-pyrazol-3-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-cyclopropyl-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-pyridin-3-yl-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-thien-2-yl-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-isoquinolin-4-yl-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(3-{[(2-hydroxyethyl)amino]carbonyl}phenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-(4-piperazin-1-ylphenyl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 1-oxo-9-vinyl-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[3-(acetylamino)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[4-(aminocarbonyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[3-({[3-(dimethylamino)propyl]amino}carbonyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[3-({[2-(dimethylamino)ethyl]amino}carbonyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(4-{[(2-hydroxyethyl)amino]carbonyl}phenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[4-(morpholin-4-ylcarbonyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-{4-[(4-methylpiperazin-1-yl)carbonyl]phenyl}-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(6-morpholin-4-ylpyridin-3-yl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(3-furyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

9-methoxy-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylic acid;

8,9-dimethoxy-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylic acid;

8-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylic acid;

9-chloro-1-oxo-8-(trifluoromethyl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxylic acid;

1-oxo-1,2-dihydro[1,3]benzodioxolo[5,6-h]isoquinoline-6-carboxylic acid;

1-oxo-1,2-dihydronaphtho[2,3-h]isoquinoline-6-carboxylic acid;

8-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carbonitrile;

8,9-dichloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carbonitrile;

methyl 9-chloro-8-methyl-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

3-(9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)propanenitrile;

6-(3-aminopropyl)-9-chlorobenzo[h]isoquinolin-1(2H)-one;

6-(2-aminoethyl)-9-chlorobenzo[h]isoquinolin-1(2H)-one;

N-(2-aminoethyl)-9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-1-oxo-9-(1H-pyrrol-2-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(3-aminopropyl)-1-oxo-9-(1H-pyrzol-4-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(3-aminopropyl)-9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-1-oxo-9-(1H-pyrrol-2-yl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-8,9-dimethoxy-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-8-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-9-chloro-1-oxo-8-(trifluoromethyl)-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-1-oxo-1,2-dihydronaphtho[2,3-h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-1-oxo-1,2-dihydro[1,3]benzodioxolo[5,6-h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-8-bromo-9-methoxy-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-8,9-dichloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-8-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

N-(2-aminoethyl)-9-methoxy-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxamide;

5-(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)propanenitrile;

6-(5-aminopropyl)-9-bromobenzo[h]isoquinolin-1(2H)-one;

3-[1-oxo-9-(1H-pyrrol-2-yl)-1,2-dihydrobenzo[h]isoquinolin-6-yl]propanenitrile;

6-(3-aminopropyl)-9-(1H-pyrrol-2-yl)benzo[h]isoquinolin-1(2H)-one; and

6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

9-[4-(aminomethyl)phenyl]-6-(3-aminopropyl)benzo[h]isoquinolin-1(2H)-one;

6-(2-cyanoethyl)-N-[3-(dimethylamino)propyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-9-carboxamide;

6-(3-aminopropyl)-9-(1H-pyrazol-5-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-9-(1-methyl-1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-9-(1H-indol-2-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-9-(1H-pyrrol-3-yl)benzo[h]isoquinolin-1(2H)-one;

3-[1-oxo-9-(1H-pyrazol-5-yl)-1,2-dihydrobenzo[h]isoquinolin-6-yl]propanenitrile;

9-bromo-6-(hydroxymethyl)benzo[h]isoquinolin-1(2H)-one;

(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)methylmethanesulfonate;

(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)acetonitrile;

6-(2-aminoethyl)-9-bromobenzo[h]isoquinolin-1(2H)-one;

6-(2-aminoethyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-aminoethyl)-9-(1H-pyrrol-2-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-aminoethyl)-9-(1H-pyrazol-5-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-aminoethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-(morpholin-4-ylmethyl)benzo[h]isoquinolin-1(2H)-one;

9-(morpholin-4-ylmethyl)-6-[4-(morpholin-4-ylmethyl)phenyl]phenanthren-4(3H)-one;

9-bromo-6-(piperazin-1-ylmethyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-({[2-(dimethylamino)ethyl]amino}methyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-{[(2-pyrrolidin-1-ylethyl)amino]methyl}benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-(1H-imidazol-1-ylmethyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[(pyrrolidin-3-ylamino)methyl]benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-(piperidin-1-ylmethyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-(pyrrolidin-1-ylmethyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[(3,3-difluoropyrrolidin-1-yl)methyl]benzo[h]isoquinolin-1(2H)-one;

6-(azetidin-1-ylmethyl)-9-bromobenzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

N-[2-(dimethylamino)ethyl]-4-[6-(hydroxymethyl)-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl]benzamide;

9-[4-(aminomethyl)phenyl]-6-(morpholin-4-ylmethyl)benzo[h]isoquinolin-1(2H)-one;

N-[3-(dimethylamino)propyl]-4-[6-(morpholin-4-ylmethyl)-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl]benzamide;

6-(azetidin-1-ylmethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-9-[4-(2-morpholin-4-ylethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(aziridin-1-ylmethyl)-9-bromobenzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[(4-fluoropiperidin-1-yl)methyl]benzo[h]isoquinolin-1(2H)-one;

6-[(3,3-difluoropyrrolidin-1-yl)methyl]-9-[4-(2-morpholin-4-ylethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

9-[4-(morpholin-4-ylmethyl)phenyl]-6-(piperidin-1-ylmethyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[(4,4-difluoropiperidin-1-yl)methyl]benzo[h]isoquinolin-1(2H)-one;

6-[(4-fluoropiperidin-1-yl)methyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-[(4,4-difluoropiperidin-1-yl)methyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(azetidin-1-ylmethyl)-9-[4-(3-hydroxypropyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(azetidin-1-ylmethyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(azetidin-1-ylmethyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-[(3,3-difluoroazetidin-1-yl)methyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-[(3,3-difluoroazetidin-1-yl)methyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[(3-fluoroazetidin-1-yl)methyl]benzo[h]isoquinolin-1(2H)-one;

6-[(3-fluoroazetidin-1-yl)methyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-[(3-fluoroazetidin-1-yl)methyl]-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(azetidin-1-ylmethyl)-9-(1H-pyrrol-2-yl)benzo[h]isoquinolin-1(2H)-one;

6-{[(2-hydroxyethyl)amino]methyl}-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-{[(2-hydroxyethyl)amino]methyl}-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(aziridin-1-ylmethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-bromo-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-(3-chlorophenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-bromo-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-phenyl-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-[4-(hydroxymethyl)phenyl]-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)-4-vinylbenzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4,9-di(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-(2-hydroxyphenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-(3-hydroxyphenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-(4-hydroxyphenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-(2-chlorophenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-[2-(hydroxymethyl)phenyl]-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-aminoethyl)-9-(4,5-dibromo-1H-pyrrol-2-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-aminoethyl)-9-(3,4,5-tribromo-1H-pyrrol-2-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-4-(2-fluorophenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(3-fluorophenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(4-fluorophenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)-4-[3-(trifluoromethyl)phenyl]benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)-4-[4-(trifluoromethyl)phenyl]benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(1H-indol-5-yl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(2-methoxyphenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(3-methoxyphenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(4-methoxyphenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-cyclohex-1-en-1-yl-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(1-benzofuran-2-yl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)-4-(1H-pyrrol-2-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)-4-(1H-pyrrol-2-yl)benzo[h]isoquinoline-1(2H)-one;

4-(4-aminophenyl)-6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(1H-indazol-5-yl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

tert-butyl 3-[6-(3-aminopropyl)-1-oxo-9-(1H-pyrazol-4-yl)-1,2-dihydrobenzo[h]isoquinoline-4-yl]-1H-indole-1-carboxylate;

6-(3-aminopropyl)-4-(2,4-dichlorophenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-9-(1H-pyrazol-4-yl)-4-[2-(trifluoromethyl)phenyl]benzo[h]isoquinoline-1 (2H)-one;

6-(3-aminopropyl)-4-(1-phenylvinyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

6-(3-aminopropyl)-4-(1,3-benzodioxol-5-yl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinoline-1(2H)-one;

4-bromo-6-(hydroxymethyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-4-(4-hydroxyphenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

4-(3-chlorophenyl)-6-(hydroxymethyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

methyl 4-[4-(aminomethyl)phenyl]-9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 4-[3-(aminomethyl)phenyl]-9-chloro-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

6-(3-aminopropyl)-4-(4-chlorophenyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-4-(2-hydroxyphenyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

4-(2-chlorophenyl)-6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

4-(2-fluorophenyl)-6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-4-(2-methylphenyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

4-(4-chlorophenyl)-6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]-4-[2-(trifluoromethoxy)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-4-(2-methoxyphenyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-4-(4-methylphenyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]-4-(1-propyl-1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

4-cyclohex-1-en-1-yl-6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

4-(3,5-dimethylisoxazol-4-yl)-6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

4-(3-chlorophenyl)-6-(hydroxymethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-4-[4-(3-hydroxypropyl)phenyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(hydroxymethyl)-4-[3-(3-hydroxypropyl)phenyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

methyl 9-(3-formylphenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(3-{[[3-(dimethylamino)propyl](methyl)amino]methyl}phenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(3-{[[2-(dimethylamino)ethyl](methyl)amino]methyl}phenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(4-{[[2-(dimethylamino)ethyl](methyl)amino]methyl}phenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-(4-{[[3-(dimethylamino)propyl](methyl)amino]methyl}phenyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[3-({[2-(dimethylamino)ethyl]amino}methyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

methyl 9-[4-({[2-(dimethylamino)ethyl]amino}methyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

6-(3-aminopropyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-9-carbonitrile;

6-(3-aminopropyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-9-carboxamide;

6-(2-aminoethyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-9-carbonitrile;

(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)acetic acid;

9-bromo-6-(2-hydroxyethyl)benzo[h]isoquinolin-1(2H)-one;

2-(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)ethylmethanesulfonate;

9-bromo-6-(2-morpholin-4-ylethyl)benzo[h]isoquinolin-1(2H)-one;

3-(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)propanamide;

9-bromo-6-(2-pyrrolidin-1-ylethyl)benzo[h]isoquinolin-1(2H)-one;

6-[2-(4-acetylpiperazin-1-yl)ethyl]-9-bromobenzo[h]isoquinolin-1(2H)-one;

6-{2-[(2-aminoethyl)amino]ethyl}-9-bromobenzo[h]isoquinolin-1(2H)-one;

6-{2-[(3-aminopropyl)amino]ethyl}-9-bromobenzo[h]isoquinolin-1(2H)-one;

9-bromo-6-(2-{[2-(4-methylphenyl)ethyl]amino}ethyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[2-(methylamino)ethyl]benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-{2-[(4-fluorobenzyl)amino]ethyl}benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[2-(dimethylamino)ethyl]benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-{2-[(4-methylbenzyl)amino]ethyl}benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[2-(ethylamino)ethyl]benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-{2-[(2-pyridin-3-ylethyl)amino]ethyl}benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-(2-{[2-(4-fluorophenyl)ethyl]amino}ethyl)benzo[h]isoquinolin-1(2H)-one;

9-bromo-6-[2-({2-[4-(trifluoromethyl)phenyl]ethyl}amino)ethyl]benzo[h]isoquinolin-1(2H)-one;

6-(2-azetidin-1-ylethyl)-9-bromobenzo[h]isoquinolin-1(2H)-one;

9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-5-carbonitrile;

N-(2-aminoethyl)-9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-5-carboxamide;

N-(3-aminopropyl)-9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinoline-5-carboxamide;

9-bromo-5-(hydroxymethyl)benzo[h]isoquinolin-1(2H)-one;

5-{[(2-aminoethyl)amino]methyl}-9-bromobenzo[h]isoquinolin-1(2H)-one;

5-{[(3-aminopropyl)amino]methyl}-9-bromobenzo[h]isoquinolin-1(2H)-one;

9-bromo-5-[(pyrrolidin-3-ylamino)methyl]benzo[h]isoquinolin-1(2H)-one;

3-[9-(1H-imidazol-1-yl)-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl]propanenitrile;

6-(3-aminopropyl)-9-(1H-imidazol-1-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-9-(1H-1,2,3-triazol-1-yl)benzo[h]isoquinolin-1(2H)-one;

6-(3-aminopropyl)-9-(2H-1,2,3-triazol-2-yl)benzo[h]isoquinolin-1(2H)-one;

(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)(difluoro)acetonitrile;

2-(9-bromo-1-oxo-1,2-dihydrobenzo[h]isoquinolin-6-yl)-2,2-difluoroethanamine;

6-(2-amino-1,1-difluoroethyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-amino-1,1-difluoroethyl)-9-(1H-pyrrol-2-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-amino-1-fluoroethyl)-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-(2-amino-1-fluoroethyl)-9-bromobenzo[h]isoquinolin-1(2H)-one;

6-(2-amino-1-fluoroethyl)-9-(1-methyl-1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-{3-[(4-fluorobenzyl)amino]propyl}-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-{3-[(4-fluorobenzyl)amino]propyl}-9-(1H-pyrrol-2-yl)benzo[h]isoquinolin-1(2H)-one;

6-[3-(isobutylamino)propyl]-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-[3-(diisobutylamino)propyl]-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

4-{6-[3-(neopentylamino)propyl]-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl}1-H-pyrazol-1-ium;

4-{6-[3-(dimethylamino)propyl]-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl}-1H-pyrazol-1-ium;

4-{6-[3-(ethylamino)propyl]-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl}-1H-pyrazol-1-ium;

4-{6-[3-(diethylamino)propyl]-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl}-1H-pyrazol-1-ium;

4-(6-{3-[(4-methylbenzyl)amino]propyl}-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl)-1H-pyrazol-1-ium;

4-[6-(3-{[2-(4-methylphenyl)ethyl]amino}propyl)-1-oxo-1,2-dihydrobenzo[h]isoquinolin-9-yl]-1H-pyrazol-1-ium;

6-{2-[(4-fluorobenzyl)amino]ethyl}-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-{2-[bis(4-fluorobenzyl)amino]ethyl}-9-(1H-pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one;

6-{2-[(4-fluorobenzyl)amino]ethyl}-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-{2-[bis(4-fluorobenzyl)amino]ethyl}-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

9-[4-(morpholin-4-ylmethyl)phenyl]-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carbaldehyde;

6-(1-hydroxyethyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-(1-hydroxypropyl)-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one;

6-[hydroxy(pyridin-2-yl)methyl]-9-[4-(morpholin-4-ylmethyl)phenyl]benzo[h]isoquinolin-1(2H)-one; and

methyl 9-chloro-8-(hydroxymethyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-6-carboxylate;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

8 . A pharmaceutical composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of a compound of claim 1 .

9 . A method of treating or prevention of cancer comprising the step of administering to a mammal a therapeutically effective amount of compound of claim 1 .

10 . (canceled)