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. Author manuscript; available in PMC: 2015 Feb 1.
Published in final edited form as: Cancer Treat Rev. 2013 Jul 5;40(1):10.1016/j.ctrv.2013.05.009. doi: 10.1016/j.ctrv.2013.05.009

Table 5.

DNA Methyl Transferase Inhibitors: Mode of inhibition and Current Status.

DNMTi COMPOUND NAMES DNMT
SPECIFICITY		 STATUS REF
NUCLEOSIDE ANOLOGUES
graphic file with name nihms-491539-t0021.jpg Azacitine
(5-Aza-CR)		 DNA
DNMT ADUCTs		 APPROVED 96
graphic file with name nihms-491539-t0022.jpg Decitabine
(5-Aza-CdR)		 DNA/RNA
DNMT ADUCTs		 APPROVED 96
graphic file with name nihms-491539-t0023.jpg Zebularine DNA/RNA
DNMT ADUCTs		 Preclinical 102-109
graphic file with name nihms-491539-t0024.jpg 5-Fluoro-
deoxycytidine
(FdCyd/FDAC)		 DNA/RNA
DNMT ADUCTs		 Phase I/II 111-114
NON-NUCLEOSIDE ANOLOGUES
graphic file with name nihms-491539-t0025.jpg Procaine DNMT1 Phase I 115
graphic file with name nihms-491539-t0026.jpg Procanamide DNMT1 Phase I 119
graphic file with name nihms-491539-t0027.jpg Hydralazine DNMT1,
DNMT3A & 3B		 Phase II/III 116-118
graphic file with name nihms-491539-t0028.jpg RG108 DNMT1 IC50 = 1000μM 121

Red circles denote unique atoms or side groups relative to the parent compound.