Research Article

D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity

Table 1

Calculated IC50 values for the compounds tested (8a–i) towards MCF7, HCT116, JURKAT, and NCI-H460 cells for a 48 h period. Standard errors are given within parentheses.

CompoundsIC50 (μM; 48 h)
MCF7HCT116JURKATNCI-H460

8a213.56 (±3.45)128.36 (±4.07)148.54 (±2.75)186.43 (±3.15)
8b337.86 (±4.70)132.34 (±2.04)261.89 (±3.45)280.51 (±2.25)
8c335.65 (±2.25)134.43 (±3.94)146.78 (±3.15)172.78 (±1.95)
8d304.12 (±3.25)144.16 (±3.45)147.23 (±2.25)221.89 (±3.85)
8e324.54 (±3.80)133.12 (±3.95)158.45 (±2.40)219.63 (±2.45)
8f98.54 (±2.65)68.60 (±3.35)76.46 (±2.45)84.47 (±2.15)
8g146.54 (±3.75)129.87 (±2.45)176.99 (±3.25)188.65 (±3.45)
8h87.65 (±2.55)57.35 (±2.45)69.12 (±2.07)76.36 (±2.65)
8i140.73 (±3.07)148.56 (±3.00)128.45 (±2.15)176.54 (±1.27)
CPT41.59 (±3.85)40.27 (±3.05)41.48 (±3.15)42.61 (±2.45)