Table 3. SAR Combination and Lead Optimization on the Indazole-Substituted Pyrimidine-2,4-dione Scaffold.
Activity data based on n ≥ 3 with SEM within 0.2 log units, unless otherwise stated.
LLE = pIC50 – log D.
NCI-H1993 cell lines; activity data based on n ≥ 3 with SEM within 0.2 log units, unless otherwise stated.
Log D measured via shake-flask method in octanol and water at pH7.4.
n = 2.
SEM = 0.22 log units.