Table 1.

Evaluation of 5,5′ substituted Apogossypol derivatives using a combination of one-dimensional 1H-NMR binding assays, competitive FPAs, and cell viability assays

Embedded Image
CompoundROne-dimensional 1H-NMR binding assay*, Bcl-XLFPA IC50 (μmol/L), Bcl-XLPC3ML EC50 (μmol/L)H460 EC50 (μmol/L)H1299 EC50 (μmol/L)RS11846 EC50 (μmol/L)RS11846 EC50 (μmol/L)
GossypolEmbedded Image++2.723.13.06.02.24.23
ApogossypolEmbedded Image++3.6910.35.83.45.08.6
BI79F5H+ND12.610.113.410.024.7
BI79D1Embedded Image++ND3.91.54.81514.7
BI79D3Embedded Image+1.307.51.13.61013.7
BI79D11Embedded Image+1.293.01.53.02.86.6
BI79D8Embedded Image+0.453.41.13.14.04.5
BI79D6Embedded Image+2.93.60.314.2ND18.3
BI79D9Embedded Image+0.163.00.592.41.84.2
BI79D12Embedded ImageND7.78.29.62.825.9
BI79F3Embedded ImageND2.83.64.82.313.4
BI79F4Embedded Image+0.252.92.22.02.53.8
BI79D10Embedded Image+++0.194.60.683.52.64.9
BI79F7Embedded Image++0.322.50.821.72.23.0
BI79F11Embedded Image++1.313.12.72.68.45.3
BI79F12Embedded Image++1.301.93.33.91.86.2
BI79F8Embedded Image+NR1.91.82.125.2
BI79F6Embedded Image++0.142.81.52.22.33.1
BI79D7Embedded Image+0.395.21.45.82.97
BI79D2Embedded Image++NRNRNRNRNR14.7
BI79D5Embedded Image+NRNRNRNRNR17.1
BI79D4Embedded Image+NRNRNRNRNR11.7
  • *Four-point rating scale: +++, very active; ++, active; +, mild; −, weak.

  • Compounds against RS11846 cell line using ATP-LITE assay.

  • Compounds against RS11846 cell line using Annexin V-FITC and PI assay.