Table 1.
Cmpd | R | R1 | % Inhib. @ 2 µM |
IC50 (nM) |
---|---|---|---|---|
2 | H | Me | 82 | 537 |
11a | (±)-Me | Me | 46 | ND |
11b | (±)-Et | Me | 27 | ND |
11c | (±)-Et | Et | 45 | ND |
11d | (±)-Me | Et | 57 | ND |
11e | (±)-Me | 87 | 570 | |
11f | a(±)-Me | ND | 152 | |
11g | a(−)-Me | ND | 1,900 | |
11h | (±)-Et | 84 | 756 | |
11i | a(+)-Et | ND | 385 | |
11j | a(−)-Et | 40 | ND | |
11k | H | ND | 61 | |
11m | H | ND | 177 | |
11n | H | ND | 1057 |
ND: not determined.
enantiomers separated by chiral SFC and (+) or (−) rotation noted,19 absolute stereochemistry is unknown.