Table 2.

The inhibitory potency of uridine-derived nucleotides 4a-y as rat CD73 inhibitors. R², X, Y = H, W = O, V = CH, Z = N, n = 1, unless otherwise noted.

Compd.	Substitution	R1	R2	Ki ± SEM (nM) (% inhibition at indicated concentration), rat CD73
UOPCP 4a		OH	H	1830 ± 530
4b	Y = CH3	OH	H	1860 ± 400
4c	Y = C2H5	OH	H	> 1000 (4%)
4d	Y = C3H7	OH	H	> 1000 (7%)
4e	Y = benzyl	OH	H	> 1000 (3%)
4f	X = CH3	OH	H	338 ± 56
4g	X = CH3	H	H	639 ± 65
4h	X = CH3	OCH3	H	> 1000 (3%)
4i	X = ethynyl	OH	H	276 ± 37
4j	X = 1-chlorovinyl	OH	H	424 ± 27
4k	X = 1-chlorovinyl, Y = CH3	OH	H	1050 ± 290
4l	X = F	OH	H	14.8 ± 1.9
4m	X = Cl	OH	H	86.7 ± 7.6
4n	X = Br	OH	H	88.7 ± 12.5
4o	X = I	OH	H	162 ± 4
4p		H	H	> 1000 (37%)
4q		NH2	H	> 1000 (2%)
4r		N3	H	> 1000 (9%)
4s		F	H	> 1000 (11%)
4t		H	F	1750± 380
4u		H	OH	> 1000 (8%)
4v	V = N	OH	H	> 1000 (21%)
4w	n = 2	OH	H	> 1000 (4%)
4x	n= 2, X = CH3	OH	H	> 1000 (9%)
4y	W = S	OH	H	> 1000 (7%)