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. Author manuscript; available in PMC: 2008 Sep 15.
Published in final edited form as: J Med Chem. 2007 Jul 18;50(16):3906–3920. doi: 10.1021/jm070311l

Table 2.

Inhibitory activities of compounds with different ring systems at the 4- and 8-positions

graphic file with name nihms62594f6.jpg
Comp. Type R1 ENT1 inhibitory activity in K562 cells determined by flow cytometry
%Inhibition at 10μM IC50 (nM) Ki (nM)
DMSO - - 0.0 ± 0.7 N. D.a N. D.
NBMPR - - 97.1 ± 0.4 7.6 0.43
Lidoflazine - - 90.0 ± 0.2 4954 279.9
Dipyridamole A graphic file with name nihms62594t1.jpg 86.7 ± 0.1 144.8 8.18
1 B 53.5 ± 0.1 12,229 690.9
2 A graphic file with name nihms62594t2.jpg 85.7 ± 0.3 1,764 99.7
3 B 19.3 ± 1.1 ND ND
4 A graphic file with name nihms62594t3.jpg 70.4 ± 0.4 6,956 393
5 B 13.5 ± 0.3 ND ND
6 A graphic file with name nihms62594t4.jpg 0.9 ± 0.7 ND ND
7 A graphic file with name nihms62594t5.jpg 44.6 ± 2.1 ND ND
8b A - 68.8 ± 0.0 7,947 449
9 A graphic file with name nihms62594t6.jpg N. D. ND ND
10 A graphic file with name nihms62594t7.jpg N. D. ND ND
11 A graphic file with name nihms62594t8.jpg 94.4 ± 0.2 15.2 0.86
12 B 28.7 ± 0.1 ND ND
13 A graphic file with name nihms62594t9.jpg 93.1 ± 0.3 8.67 0.49
14 B 78.6 ± 0.3 375 21.2
15 A graphic file with name nihms62594t10.jpg 78.0 ± 0.4 13.6 0.77
16 B 69.3 ± 0.3 672 38
17 A graphic file with name nihms62594t11.jpg 85.0 ± 0.1 3,416 193
18 B 14.9 ± 1.7 ND ND
19 A graphic file with name nihms62594t12.jpg 24.7 ± 0.2 ND ND
20 B 16.2 ± 1.9 ND ND
a

ND = Not Determined.

b

For structure of compound 8, see Scheme 1.