TABLE 1.

Structure–Activity Relationships of Quinazolinone Derivatives

CompoundIC50 (nM)pIC50*cLog D7.4
4a353.1−0.08
4b19.87.72 ± 0.110.74
5a40.17.43 ± 0.170.89
5b2.38.65 ± 0.031.76
7a17.67.76 ± 0.051.55
7b (LCE470)0.339.49 ± 0.092.53
  • * Mean value ± SEM.

  • Calculated using ACD/Labs software.

  • IC50 = half-maximum inhibitory concentration; pIC50 = negative log of the IC50 value in molar concentration; cLog D7.4 = calculated log distribution coefficient.