Table 1.

Structure, log P value, stability, and pharmacokinetics of DAC and 5′-O-trialkylsilylated DACs

		DAC	OR-2003	OR-2009	OR-2100	OR-2102
	R 1	H	H	H	H	H
	R 2	H	H	H	H	H
	R3 = R4	H	H	H	H	H
	R 5	–	Methyl	Methyl	Ethyl	Ethyl
	R 6	–	Methyl	Methyl	Ethyl	Ethyl
	R 7	–	n-Propyl	c-Hexyl	Ethyl	n-Propyl
Log P value		− 0.32	1.64	2.52	2.14	2.54
Stability	t1/2 in PBS	20 h*	20** + 1 h	20** + 14 h	20** + 16 h	20** + 19 h
	Enzymatic	Complete degradation after 0.5 h	Retain 52% after 1 h	Retain 75% after 2 h	Retain 84% after 2 h	Retain 46% after 2 h
AUC 0 → lim (μM·hr)	OR compound	—	0.305	0.314	0.168	0.081
	DAC	0.378	0.338	0.238	0.266	0.285
	Total	0.378	0.643	0.552	0.434	0.366

DAC decitabine, PBS phosphate-buffered saline

*Reference: Yoo C.B. et al. Cancer Research 2007; 67:6400–6408

**20 h: t_1/2 in PBS of DAC