Table 1. Activity of MS-0022 and deletion/substitution analogs (See structure in figure 1A).
ID | R1 | R2 | R3 | MW | IC50 (Shh-L2, nM) |
MS-0022 | 8-methylimidazo[1,2-a]pyridine | – | 2-bromophenyl | 406.3 | 100 |
MS-0011 | 8-methylimidazo[1,2-a]pyridine | – | Methyl | 265.3 | >20,000 |
MS-0012 | 8-methylimidazo[1,2-a]pyridine | – | 2-propyl | 293.4 | >20,000 |
MS-0013 | – | O-Amide | 2-bromophenyl | 319.2 | >20,000 |
MS-0014 | Propyl | – | 2-bromophenyl | 318.2 | 10,000 |
MS-0015 | 6-morpholinopyridazin-3-yl | – | 2-bromophenyl | 439.3 | 800 |
MS-0016 | (6-phenylpyrimidin-4-yl)amino | – | 2-bromophenyl | 445.3 | 2000 |
MS-0017 | naphthalen-2-ylcarbamoyl | – | 2-bromophenyl | 445.3 | 280 |
MS-0018 | 2-benzylidenehydrazinecarbonyl | – | 2-bromophenyl | 442.3 | 5000 |
Table depicting molecular weight and bological activity (nM IC50) of deletion or substitution analogs of MS-0022 as measured by pathway inhibition in Shh induced Shh-L2 cells.