Inhibitors of histone deacetylase

1. A compound represented by Formula I:

wherein

X is 1) —(CR 2 2 ) n C(O)OR 1 ,

2) —(CR 2 2 ) n C(O)NR 1 2 ,

3) —(CR 2 2 ) n C(O)R 1 ,

4) —(CR 2 2 ) n OC(O)NR 1 2 ,

5) —(CR 2 2 ) n aryl, wherein aryl is optionally substituted with one or more substituents,

6) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) m NR 1 2 ,

7) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) m NR 1 C(O)R 1 ,

8) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) n OR 1 , or

9) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) n C(O)NR 1 2 ;

Y is unsubstituted or substituted aryl or unsubstituted or substituted thienyl or pyridinyl;

Z is aryl or heteroaryl;

R is H or unsubstituted or substituted C 1 -C 6 alkyl;

R 1 is independently selected from H, C 1 -C 6 alkyl, —(CR 2 2 ) n aryl, and —(CR 2 2 ) n heterocyclyl;

wherein said alkyl, aryl or heterocyclyl is optionally substituted with one or more substituents;

R 2 and R 3 are independently selected from H, unsubstituted or substituted C 1 -C 6 alkyl, and (CR 2 2 ) n aryl;

R 4 is

1) —(CR 2 2 ) n NR 5 2 ,

2) —(CR 2 2 ) n NR 5 C(O)R 5 ,

3) —(CR 2 2 ) n NR 5 C(O)OR 5 ,

4) —(CR 2 2 ) n heterocyclyl,

5) —(CR 2 2 ) n NR 5 S(O) 2 R 5 , or

6) —(CR 2 2 ) n NR 5 C(O)NR 5 2 ;

wherein heterocyclyl is optionally substituted with one or more substituents;

optionally, when R is unsubstituted or substituted C 1 -C 6 alkyl and R 4 is not —(CR 2 2 ) n heterocyclyl, R and R 4 may be cyclized to form a ring system;

R 5 is independently selected from H, C 1 -C 6 alkyl, —(CR 2 2 ) n aryl, and —(CR 2 2 ) n heterocyclyl, wherein alkyl, aryl or heterocyclyl may be optionally substituted with one or more substituents;

R 8 is unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl;

R 12 is NH 2 , NR 5 C(O)R 5 , NR 5 C(O)OR 5 , OH, or NH-Boc;

m is 1, 2 or 3;

n is independently 0, 1, 2, 3 or 4;

p is 0, 1, 2, 3, or 4;

s is 0, 1 or 2;

or a stereoisomer or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 , wherein

Y is phenyl, thienyl, or pyridinyl, wherein phenyl, thienyl or pyridinyl is optionally substituted with one or two substituents selected from R 7 ;

Z is phenyl, pyrazolyl, thienyl or pyridinyl;

R 2 and R 3 are independently selected from H and unsubstituted or substituted C 1 -C 6 alkyl;

R 7 is independently selected from unsubstituted or substituted C 1 -C 6 alkyl, OR 5 , —(CR 2 2 ) n aryl, CN, CF 3 and halo;

or a stereoisomer or a pharmaceutically acceptable salt thereof.

3. The compound according to claim 1 , represented by Formula II

wherein

X is 1) —(CR 2 2 ) n C(O)OR 1 ,

2) —(CR 2 2 ) n C(O)NR 1 2 ,

3) —(CR 2 2 ) n C(O)R 1 ,

4) —(CR 2 2 ) n OC(O)NR 1 2 ,

5) —(CR 2 2 ) n aryl, wherein aryl is optionally substituted with one to three substituent selected from R 7 ,

6) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) m NR 1 2 ,

7) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) m NR 1 C(O)R 1 ,

8) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) n OR 1 , or

9) —(CR 2 2 ) n C(O)NR 1 (CR 2 2 ) n C(O)NR 1 2 ;

Z is phenyl or pyrazolyl;

R is H or unsubstituted or substituted C 1 -C 6 alkyl;

R 1 is independently selected from H, C 1 -C 6 alkyl, —(CR 2 2 ) n aryl, and —(CR 2 2 ) n heterocyclyl;

wherein said alkyl, aryl or heterocyclyl is optionally substituted with one to three substituent selected from R 7 ;

R 2 and R 3 are independently selected from H, unsubstituted or substituted C 1 -C 6 alkyl, and (CR 2 2 ) n aryl;

R 4 is

1) —(CR 2 2 ) n NR 5 2 ,

2) —(CR 2 2 ) n NR 5 C(O)R 5 ,

3) —(CR 2 2 ) n NR 5 C(O)OR 5 ,

4) —(CR 2 2 ) n heterocyclyl,

5) —(CR 2 2 ) n NR 5 S(O) 2 R 5 , or

6) —(CR 2 2 ) n NR 5 C(O)NR 5 2 ;

wherein heterocyclyl is optionally substituted with one to three substituent selected from R 7 ;

R 5 is independently selected from H, C 1 -C 6 alkyl, —(CR 2 2 ) n aryl, and —(CR 2 2 ) n heterocyclyl, wherein alkyl, aryl or heterocyclyl may be optionally substituted with one to three substituent selected from R 7 ;

R 7 is independently selected from unsubstituted or substituted C 1 -C 6 alkyl, OR 5 , —(CR 2 2 ) n aryl, CN, CF 3 and halo;

R 8 is unsubstituted or substituted phenyl or unsubstituted or substituted thienyl;

R 12 is NH 2 , OH, or NH-Boc;

m is 1, 2 or 3;

n is independently 0, 1, 2, 3 or 4;

p is 0, 1, 2, or 3;

s is 0, or 1;

or a stereoisomer or a pharmaceutically acceptable salt thereof.

4. The compound according to claim 1 , represented by Formula III

wherein

X is 1) —(CR 2 2 ) n C(O)OR 1 ,

2) —(CR 2 2 ) n C(O)NR 1 2 ,

3) —(CR 2 2 ) n C(O)R 5 , or

4) —(CR 2 2 ) n aryl, wherein aryl is optionally substituted with one to three substituent selected from R 7 ;

R is H or unsubstituted or substituted C 1 -C 6 alkyl;

R 1 is independently selected from H, C 1 -C 6 alkyl, —(CR 2 2 ) n aryl, and —(CR 2 2 ) n heterocyclyl;

wherein said alkyl, aryl or heterocyclyl is optionally substituted with one to three substituent selected from R 7 ;

R 2 and R 3 are independently selected from H, unsubstituted or substituted C 1 -C 6 alkyl, and (CR 2 2 ) n aryl;

R 4 is

1) —(CR 2 2 ) n NR 5 2 ,

2) —(CR 2 2 ) n NR 5 C(O)R 5 ,

3) —(CR 2 2 ) n NR 5 C(O)OR 5 ,

4) —(CR 2 2 ) n heterocyclyl,

5) —(CR 2 2 ) n NR 5 S(O) 2 R 5 , or

6) —(CR 2 2 ) n NR 5 C(O)NR 5 2 ;

wherein heterocyclyl is optionally substituted with one to three substituent selected from R 7 ;

R 5 is independently selected from H, C 1 -C 6 alkyl, —(CR 2 2 ) n aryl, and —(CR 2 2 ) n heterocyclyl, wherein alkyl, aryl or heterocyclyl may be optionally substituted with one to three substituent selected from R 7 ;

R 7 is independently selected from unsubstituted or substituted C 1 -C 6 alkyl, OR 5 , —(CR 2 2 ) n aryl, CN, CF 3 and halo;

R 8 is phenyl or thienyl;

R 12 is NH 2 ;

n is independently 0, 1, 2, 3 or 4;

p is 0, 1, 2, or 3;

or a stereoisomer or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 selected from

amino[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]acetic acid;

ethyl amino[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]acetate;

4-[1-amino-2-(methylamino)-2-oxoethyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

N-[2-amino-5-(2-thienyl)phenyl]-4-(1,2-diamino-2-oxoethyl)benzamide;

4-{1-amino-2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl}-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-{1-amino-2-[(2-methoxyphenyl)amino]-2-oxoethyl}-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)benzamide;

4-[1-amino-2-(isoxazol-3-ylamino)-2-oxoethyl]-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)benzamide;

4-[1-amino-2-oxo-2-(pyridin-2-ylamino)ethyl]-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)benzamide;

4-{1-amino-2-[(4-methyl-1,3-thiazol-2-yl)amino]-2-oxoethyl}-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)benzamide;

4-{1-amino-2-[(3-methoxyphenyl)amino]-2-oxoethyl}-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)benzamide;

4-{1-amino-2-[(4-cyanopyridin-2-yl)amino]-2-oxoethyl}-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)benzamide;

4-[1-amino-2-(2,3-dihydro-1,4-benzodioxin-6-ylamino)-2-oxoethyl]-N-(4-amino-1-phenyl-1H-pyrazol-3-yl)benzamide;

ethyl [4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]{[(pyridin-3-ylmethoxy)carbonyl]amino}acetate;

[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]{[(pyridin-3-ylmethoxy)carbonyl]amino}acetic acid;

pyridin-3-ylmethyl [1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]-2-(methylamino)-2-oxoethyl]carbamate;

pyridin-3-ylmethyl {2-amino-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino} carbonyl)phenyl]-2-oxoethyl}carbamate;

pyridin-3-ylmethyl [1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]-2-(ethylamino)-2-oxoethyl]carbamate;

pyridin-3-ylmethyl [1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]-2-(isopropylamino)-2-oxoethyl]carbamate;

pyridin-3-ylmethyl [1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]-2-(dimethylamino)-2-oxoethyl]carbamate;

(acetylamino)[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]acetic acid;

4-[1-(acetylamino)-2-oxo-2-pyrrolidin-1-ylethyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-[1-(acetylamino)-2-amino-2-oxoethyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-[1-(acetylamino)-2-(methylamino)-2-oxoethyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-[1-(acetylamino)-2-(dimethylamino)-2-oxoethyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-[1-(acetylamino)-2-(isopropylamino)-2-oxoethyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-[1-(acetylamino)-2-(ethylamino)-2-oxoethyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

Tert-butyl [2-({4-[1-(acetylamino)-2-(methylamino)-2-oxoethyl]benzoyl}amino)-4-(2-thienyl)phenyl] carbamate;

N-[2-amino-5-(2-thienyl)phenyl]-4-[2-(methylamino)-2-oxo-1-pyrrolidin-1-ylethyl]benzamide;

[4-({[2-amino-5-(2-thienyl)phenyl] amino}carbonyl)phenyl](pyrrolidin-1-yl)acetic acid;

N-[2-amino-5-(2-thienyl)phenyl]-4-[2-(isopropylamino)-1-(4-methylpiperidin-1-yl)-2-oxoethyl]benzamide;

N-(2-amino-5-thien-2-ylphenyl)-4-{1-azetidin-1-yl-2-[(4-methylphenyl)amino]-2-oxoethyl}benzamide;

N-(2-amino-5-thien-2-ylphenyl)-4-[1-(diethylamino)-2-(isopropylamino)-2-oxoethyl]benzamide;

N-(2-amino-5-thien-2-ylphenyl)-4-[1-azetidin-1-yl-2-(isopropylamino)-2-oxoethyl]benzamide;

N-(2-amino-5-thien-3-ylphenyl)-5-[2-[(4-chlorophenyl)amino]-1-(4-methylpiperazin-1-yl)-2-oxoethyl]thiophene-2-carboxamide;

N-(2-amino-5-thien-2-ylphenyl)-5-[2-[(4-chlorophenyl)amino]-1-(4-methylpiperazin-1-yl)-2-oxoethyl]thiophene-2-carboxamide;

N-(2-aminophenyl)-4-[1-(benzoylamino)-2-(benzylamino)-2-oxoethyl]benzamide;

N-(2-aminophenyl)-4-[1,2-bis(benzylamino)-2-oxoethyl]benzamide;

N-(2-aminophenyl)-4-{2-(benzylamino)-2-oxo-1-[(2-phenylethyl)amino]ethyl Benzamide;

N-(2-aminophenyl)-4-{1-(benzoylamino)-2-[(4-chlorophenyl)amino]-2-oxoethyl}benzamide;

N-(2-aminophenyl)-4-{2-[(4-chlorophenyl)amino]-2-oxo-1-[(phenylacetyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-{2-[(4-chlorophenyl)amino]-2-oxo-1-[(3-phenylpropanoyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-{1-(benzoylamino)-2-[(4-methylphenyl)amino]-2-oxoethyl}benzamide;

N-(2-aminophenyl)-4-[1-(benzoylamino)-2-(2-naphthylamino)-2-oxoethyl]benzamide;

N-(2-aminophenyl)-4-{2-[(4-methylphenyl)amino]-2-oxo-1-[(phenylacetyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-{2-[(4-methoxyphenyl)amino]-2-oxo-1-[(phenylacetyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-{2-(2-naphthylamino)-2-oxo-1-[(phenylacetyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-{2-[(4-methylphenyl)amino]-2-oxo-1-[(3-phenylpropanoyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-{2-[(4-methoxyphenyl)amino]-2-oxo-1-[(3-phenylpropanoyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-{2-(2-naphthylamino)-2-oxo-1-[(3-phenylpropanoyl)amino]ethyl}benzamide;

N-(2-aminophenyl)-4-[2-(benzylamino)-1-(4-methylpiperazin-1-yl)-2-oxoethyl]-benzamide;

N-(2-aminophenyl)-4-[2-[(4-chlorophenyl)amino]-1-(4-ethylpiperazin-1-yl)-2-oxoethyl]benzamide;

N-(2-aminophenyl)-4-[2-[(4-chlorophenyl)amino]-1-(4-methylpiperazin-1-yl)-2-oxoethyl]benzamide;

N-(2-aminophenyl)-4-[1-(4-methylpiperazin-1-yl)-2-(2-naphthylamino)-2-oxoethyl]benzamide;

N-(2-aminophenyl)-4-{2-[(4-chlorophenyl)amino]-1-[(3S)-3-methylpiperazin-1-yl]-2-oxoethyl}benzamide;

N-(2-aminophenyl)-4-[2-(2-naphthylamino)-2-oxo-1-piperazin-1-ylethyl]benzamide;

N-(2-aminophenyl)-4-[2-(2-naphthylamino)-2-oxo-1-(4-phenylpiperazin-1-yl)ethyl]benzamide;

N-(2-aminophenyl)-4-{2-(2-naphthylamino)-2-oxo-1-[4-(2-phenylethyl)piperazin-1-yl]ethyl}benzamide;

N-(2-aminophenyl)-4-[1-morpholin-4-yl-2-(2-naphthylamino)-2-oxoethyl]benzamide;

N-(2-aminophenyl)-6-{2-[(4-chlorophenyl)amino]-2-oxo-1-[(3-phenylpropanoyl)-amino]ethyl}nicotinamide;

N-(2-aminophenyl)-6-[1-(4-methylpiperazin-1-yl)-2-(2-naphthylamino)-2-oxoethyl]nicotinamide;

N-(4-aminobiphenyl-3-yl)-4-[2-[(4-chlorophenyl)amino]-1-(4-methylpiperazin-1-yl)-2-oxoethyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[2-[(4-chlorophenyl)amino]-1-(4-methylpiperazin-1-yl)-2-oxoethyl]benzamide;

N-(4-aminobiphenyl-3-yl)-6-[1-(4-methylpiperazin-1-yl)-2-(2-naphthylamino)-2-oxoethyl]nicotinamide;

N-(4-aminobiphenyl-3-yl)-6-[2-(benzylamino)-1-(4-methylpiperazin-1-yl)-2-oxoethyl]nicotinamide;

N-(4-aminobiphenyl-3-yl)-6-[2-[(4-methylphenyl)amino]-1-(4-methylpiperazin-1-yl)-2-oxoethyl]nicotinamide;

N-(4-aminobiphenyl-3-yl)-6-[2-[(4-chlorophenyl)amino]-1-(4-methylpiperazin-1-yl)-2-oxoethyl]nicotinamide;

N-(2-aminophenyl)-4-[3-[(4-chlorophenyl)amino]-2-(4-methylpiperazin-1-yl)-3-oxopropyl]benzamide;

N-(2-aminophenyl)-4-[2-(4-methylpiperazin-1-yl)-3-(2-naphthylamino)-3-oxopropyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[3-[(4-chlorophenyl)amino]-2-(4-methylpiperazin-1-yl)-3-oxopropyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[3-(benzylamino)-2-(4-methylpiperazin-1-yl)-3-oxopropyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[3-[(4-methoxyphenyl)amino]-2-(4-methylpiperazin-1-yl)-3-oxopropyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[3-[(4-methylphenyl)amino]-2-(4-methylpiperazin-1-yl)-3-oxopropyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[2-(4-methylpiperazin-1-yl)-3-(2-naphthylamino)-3-oxopropyl]benzamide;

4-{[(2-Aminophenyl)amino]carbonyl}-Nα-benzoyl-N-(4-chlorophenyl)phenyl-alaninamide;

N-(4-aminobiphenyl-3-yl)-4-[4-[(4-chlorophenyl)amino]-3-(4-methylpiperazin-1-yl)-4-oxobutyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[4-(benzylamino)-3-(4-methylpiperazin-1-yl)-4-oxobutyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[3-(4-methylpiperazin-1-yl)-4-(2-naphthylamino)-4-oxobutyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[4-[(4-methylphenyl)amino]-3-(4-methylpiperazin-1-yl)-4-oxobutyl]benzamide;

N-(4-aminobiphenyl-3-yl)-4-[4-[(4-methoxyphenyl)amino]-3-(4-methylpiperazin-1-yl)-4-oxobutyl]benzamide;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-(ethylamino)-2-oxoethyl}carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(3-thienyl)phenyl]amino}carbonyl)benzyl]-2-(ethylamino)-2-oxoethyl}carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-(methylamino)-2-oxoethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(3-thienyl)phenyl]amino}carbonyl)benzyl]-2-(methylamino)-2-oxoethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino} carbonyl)benzyl]-2-(4-methylpiperazin-1-1yl)-2-oxoethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino} carbonyl)benzyl]-2-morpholin-4-yl-2-oxoethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino} carbonyl)benzyl]-2-{[2-(dimethylamino)ethyl]amino}-2-oxoethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino} carbonyl)benzyl]-2-(benzylamino)-2-oxoethyl]carbamate;

Benzyl {(1S)-2-amino-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-oxoethyl}carbamate;

(2S)-3-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]-2-{[(benzyloxy)carbonyl]amino}propanoic acid;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-(dimethylamino)-2-oxoethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-(isopropylamino)-2-oxoethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(3-thienyl)phenyl]amino}carbonyl)benzyl]-2-oxo-2-(propylamino)ethyl]carbamate;

Benzyl [(1S)-1-[4-({[2-amino-5-(3-thienyl)phenyl]amino}carbonyl)benzyl]-2-(cyclopropylamino)-2-oxoethyl]carbamate;

Benzyl {(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-[(2-methoxylethyl)amino)-2-oxoethyl}carbamate;

Benzyl ((1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-{[2-(dimethylamino)-2-oxoethyl]amino}-2-oxoethyl)carbamate;

Benzyl {(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-[[2-(dimethylamino)-2-oxoethyl](methyl)amino]-2-oxoethyl}carbamate;

Benzyl {(1S)-2-{[2-(acetylamino)ethyl]amino}-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-oxoethyl}carbamate;

Benzyl {(1S)-2-({2-[acetyl(methyl)amino]ethyl}amino)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-oxoethyl}carbamate;

Benzyl [1(S)-(4-{[4-amino-1-phenyl-1H-pyrazol-3-yl)amino] carbonyl}benzyl)-2-(methylamino)-2-oxoethyl]carbamate;

4-[(2S)-2-(acetylamino)-3-(methylamino)-3-oxopropyl]-N-2-amino-5-(2-thienyl)phenyl]benzamide;

4-[(2S)-2-(acetylamino)-3-(4-methylpiperzin-1-yl)-3-oxopropyl]-N-2-amino-5-(2-thienyl)phenyl]benzamide;

4-[(2S)-2-(acetylamino)-3-morpholin-4-yl-3-oxopropyl]-N-2-amino-5-(2-thienyl)phenyl]benzamide;

4-[(2S)-2-(acetylamino)-3-{[2-(dimethylamino)ethyl]amino}-3-oxopropyl]-N-2-amino-5-(2-thienyl)phenyl]benzamide;

4-[(2S)-2-(acetylamino)-3-(ethylamino)-3-oxopropyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-[(2S)-2-(acetylamino)-3-(benzylamino)-3-oxopropyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

N-[2-amino-5-(2-thienyl)phenyl]-4-{(2S)-2-[(methylsulfonyl)amino]-3-morpholin-4-yl-3-oxopropyl}benzamide;

N-[2-amino-5-(2-thienyl)phenyl]-4-{(2S)-3-(ethylamino)-2-[(methylsulfonyl)amino]-3-oxopropyl}benzamide;

N-[2-amino-5-(2-thienyl)phenyl]-4-{(2S)-3-(benzylamino)-2-[(methylsulfonyl)amino]-3-oxopropyl}benzamide;

pyridin-3-ylmethyl[(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-(ethylamino)-2-oxoethyl]carbamate;

pyridin-3-ylmethyl[(1S)-1-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)benzyl]-2-(methylamino)-2-oxoethyl]carbamate;

N-[(1S)-1-[4-({[2-amino-5-(3-thienyl)phenyl]amino}carbonyl)benzyl]-2-oxo-2-(propylamino)ethyl]thiophene-2-carboxamide;

4-[(2S)-2-amino-3-(ethylamino)-3-oxopropyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-[(2S)-2-amino-3-(methylamino)-3-oxopropyl]-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-((2S)-2-amino-3-{[2-(dimethylaminoethyl]amino}-3-oxopropyl)-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

4-{(2S)-2-amino-3-[(2-methoxyethyl)amino]-3-oxopropyl}-N-[2-amino-5-(2-thienyl)phenyl]benzamide;

2-amino-3-[4-({[2-amino-5-(3-thienyl)phenyl]amino}carbonyl)phenyl]propanoic acid;

Ethyl 3-[4-({[2-amino-5-(2-thienyl)phenyl]amino}carbonyl)phenyl]-2-(dimethylamino)propanoate;

4-[1-(acetylamino)-2-amino-2-oxoethyl]-N-[2-(acetylamino)-5-(2-thienyl)phenyl]benzamide;

N-[2-amino-5-(2-thienyl)phenyl]-4-{2-(methylamino)-1-[(methylsulfonyl)amino]-2-oxoethyl}benzamide;

N-[2-amino-5-(2-thienyl)phenyl]-4-(2-(methylamino)-1-{[(methylamino)carbonyl]amino}-2-oxoethyl)benzamide;

4-{1-[(Acetylamino)methyl]-2-anilino-2-oxoethyl}-N-[2-amino-5-(3-thienyl)phenyl]benzamide;

N-[2-Amino-5-(3-thienyl)phenyl]-4-[2-anilino-1-({[(methylamino)carbonyl]amino} methyl)-2-oxo-ethyl]benzamide;

N-[2-Amino-5-(3-thienyl)phenyl]-4-{2-anilino-1-[(dimethylamino)methyl]-2-oxoethyl}benzamide;

4-{1-[(acetylamino)methyl]-2-anilino-2-oxoethyl}-N-[2-amino-5-(3-thienyl)phenyl]benzamide;

4-[1-[(acetylamino)methyl]-2-(methylamino)-2-oxoethyl]-N-[2-amino-5-(3-thienyl)phenyl]benzamide;

4-[1-[(acetylamino)methyl]-2-(dimethylamino)-2-oxoethyl]-N-[2-amino-5-(3-thienyl)phenyl]benzamide;

4-{1-[(acetylamino)methyl]-2-morpholin-4-yl-2-oxoethyl}-N-[2-amino-5-(3-thienyl)phenyl]benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-{2-anilino-1-[(dimethylamino)methyl]-2-oxoethyl}benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-[1-[(dimethylamino)methyl]-2-(methylamino)-2-oxoethyl]benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-(2-anilino-1-{[(methylsulfonyl)amino]methyl}-2-oxoethyl)benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-(2-(methylamino)-1-{[(methylsulfonyl)amino]methyl}-2-oxoethyl)benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-(2-(dimethylamino)-1-{[(methylsulfonyl)amino]methyl}-2-oxoethyl)benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-[2-anilino-1-({[(methylamino)carbonyl]amino}methyl)-2-oxoethyl]benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-[2-(methylamino)-1-({[(methylamino)carbonyl]amino}methyl)-2-oxoethyl]benzamide;

N-[2-amino-5-(3-thienyl)phenyl]-4-[2-(dimethylamino)-1-({[(methylamino)carbonyl]amino}methyl)-2-oxoethyl]benzamide; and

[4-({[2-[(tert-butoxycarbonyl)amino]-5-(2-thienyl)phenyl]amino}carbonyl)phenyl] (pyrrolidin-1-yl)acetic acid;

or a stereoisomer or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition comprising a pharmaceutically effective amount of the compound according to claim 1 , and a pharmaceutically acceptable carrier.

7. A method of treating neoplastic cancer or tumor in a mammal comprising the step of administering a therapeutically effective amount of the compound of claim 1 in the mammal.