Table 1.

Assessment of in vitro and cellular potency of synthesized compounds(A) In vitro IC50 values of SCH900776 and its analogues (both enantiomeric forms), obtained from Eurofins Kinase Profiler service

CompoundIC50 (nmol/L)
SCH9007765
ent-SCH900776>300
MU377>300
ent-MU377>300
MU37828
ent-MU378>300
MU3802
ent-MU38099
(B) EC50 values of the tested compounds alone and in combination with HU
CompoundEC50 (μmol/L) mean ± SD (n = 3)
MU3800.80 ± 0.08
MU380 + HU0.33 ± 0.06
SCH9007763.57 ± 0.20
SCH900776 + HU1.39 ± 0.17
MU3784.92 ± 0.36
MU378 + HU2.73 ± 0.35
  • Abbreviation: HU, hydroxyurea.