ORIGINAL ARTICLEEvodiamine-inspired dual inhibitors of histone deacetylase 1 (HDAC1) and topoisomerase 2 (TOP2) with potent antitumor activity
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Graphical abstract
Evodiamine derivative 30a is a dual-selective inhibitor against histone deacetylase 1 (HDAC1) and topoisomerase 2 (TOP2), which possesses excellent in vivo antitumor activity in the HCT116 xenograft model without significant toxicity.
Key words
Evodiamine
Histone deacetylase
Topoisomerase
Dual inhibitors
Antitumor activity
Abbreviations
BSA
bovine serum albumin
CCK-8
cell counting kit-8
CPT
camptothecin
DIPEA
N,N-diisopropylethylamine
DMF
dimethylformamide
Eto
etoposide
HATU
1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxid hexafluorophosphate
HDAC
histone deacetylase
IP
intraperitoneal injection
OD
optical density
PI
propidium iodide
SD
Sprague–Dawley
SDS
sodium dodecyl sulfate
TAE
Tris-acetate-EDTA
TGI
tumor growth inhibition
TOP
topoisomerase
ZBG
zinc-binding group
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