Table 4.
Comp. (WL) | R3 | hENT1 IC50 (nM) | hENT2 IC50 (nM) | hENT4 IC50 (nM) |
72 | OCH2CH2OH | 289.6 | 1,785 | - |
73 | 1,638 | N.D. | N. D. | |
74 | N(CH2CH2OOCH)2 | 69.1 | 532 | N. D. |
75 | N(CH2CH2OOCCH3)2 | 238 | 708 | 14125 |
76 | N(CH2CH2OCH3)2 | 207.7 | 1,470 | 1820 |
77 | N(CH2CH2OCH2CH3)2 | 767.7 | N.D. | 29854 |
78 | N(CH2CH2OCH2CH2CH3)2 | N.D. | N.D. | 139637 |
79 | 67.5 | 175 | N. D. |
Compound 8