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. Author manuscript; available in PMC: 2020 Apr 11.
Published in final edited form as: J Med Chem. 2019 Mar 21;62(7):3677–3695. doi: 10.1021/acs.jmedchem.9b00164

Table 3.

The inhibitory potency of cytosine derivatives 7a-f and 9a-i at rat CD73.

graphic file with name nihms-1028401-t0015.jpg
Compd. Substitution R1 R2 Ki ± SEM (nM) (% inhibition at indicated concentration) rat CD73
COPCP 7a OH H 898 ± 63
7b H H > 1000 (18%)
7c X = I OH H 502 ± 83
7d X = F OH H 349 ± 41
7e X = CH3 OH H 2030 ± 670
7f OH benzoyl 13.9 ± 1.6
9a OH CH3 257 ± 39
9b OH benzyl 112 ± 15
9c H benzyl 780 ± 15
9d OH 4-trifluoromethylbenzyl 30.3 ± 4.2
9e OH naphth-2-ylmethyl 18.8 ± 3.2
9f X = CH3 OH benzyl 321 ± 9
9g X = F OH benzyl 85.1 ± 7.5
9h Y = CH3 OH benzyl 3.67 ± 0.26
9i Y = C2H5 OH benzyl 262 ± 46