Table 3
The second generation of epi-drugs
Drug name
Chemical structure
Target
a
Disease condition
b
Reference
GSK126
NH
O
H
N
O
N
N
N
HN
EZH2
Relapsed/refractory DLBCL, transformed follicular
lymphoma, other non-Hodgkin’s lymphomas, solid
tumors, and multiple myeloma
[35–37]
C646
COOH
O
2 N
N
N
O
O
p300
Abrogates TSA-induced acetylation in cells,
radiosensitizes NSCLC, potent anti-influenza virus
candidate
[38–40]
EPZ004777
O
N
HO
OH
N
N
H
N
H
O
N
N
N
DOT1L
Induces apoptosis, cell cycle arrest, and terminal
differentiation in DNMT3A-mutant human AML cells,
induces apoptosis in MLL-rearranged leukemia cells
[41, 42]
(continued)
Integrated Chemoinformatics Approaches …
253
The second generation of epi-drugs
Drug name
Chemical structure
Target
a
Disease condition
b
Reference
GSK126
NH
O
H
N
O
N
N
N
HN
EZH2
Relapsed/refractory DLBCL, transformed follicular
lymphoma, other non-Hodgkin’s lymphomas, solid
tumors, and multiple myeloma
[35–37]
C646
COOH
O
2 N
N
N
O
O
p300
Abrogates TSA-induced acetylation in cells,
radiosensitizes NSCLC, potent anti-influenza virus
candidate
[38–40]
EPZ004777
O
N
HO
OH
N
N
H
N
H
O
N
N
N
DOT1L
Induces apoptosis, cell cycle arrest, and terminal
differentiation in DNMT3A-mutant human AML cells,
induces apoptosis in MLL-rearranged leukemia cells
[41, 42]
(continued)
Integrated Chemoinformatics Approaches …
253