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. 2014 Dec 23;15(12):1688–1699. doi: 10.4161/15384047.2014.972799

Table 1.

Chemical structures of maritoclax derivatives bearing a pyoluteorin motif. Viability of U937 cells treated with the indicated compounds over 48 hours were used to calculate the EC50 values. For additional compounds that deviate from the pyoluteorin motif, see Table S1

Pyoluteorin Motif Compound X Y Z R1 R2 R3 EC50 (μM)
graphic file with name kcbt-15-12-972799-i001.gif KS01 ‒H ‒OCH3 ‒H ‒H ‒H ‒H > 50
KS02 ‒H ‒OH ‒H ‒H ‒H ‒H 19
KS03 ‒Br ‒OCH3 ‒H ‒H ‒H ‒H > 50
KS04 ‒Br ‒OH ‒H ‒H ‒H ‒H 1.7
KS05 ‒Br ‒OCH3 ‒Br ‒H ‒H ‒H 13
KS06 ‒Br ‒OH ‒Br ‒H ‒H ‒H 11
KS07 ‒H ‒OCH3 ‒H ‒OCH3 ‒OCH3 ‒H > 50
KS08 ‒H ‒OH ‒H ‒OCH3 ‒OCH3 ‒H 30
  KS09 ‒H ‒OH ‒H ‒OH ‒OH ‒H 33
  KS11 Br ‒OCH3 ‒H ‒OCH3 ‒OCH3 ‒H 22
  KS12 Br ‒OH ‒H ‒OH ‒OCH3 ‒H 5.0
  KS13 ‒CH3 ‒OH ‒H ‒H ‒H ‒H 13
  KS14 ‒Br ‒OH ‒H ‒H ‒OH ‒H 30
  KS17 ‒Br ‒OCOCH3 ‒H ‒H ‒H ‒H 1.8
  KS18 ‒Br ‒OH ‒H ‒H ‒H ‒Cl 0.5
  KS18a ‒Br ‒OPO3H2 ‒H ‒H ‒H ‒Cl 3.3
  KS19 ‒Br ‒OCOCH3 ‒H ‒H ‒H ‒Cl 0.5
  KS20 ‒Br ‒OH ‒H ‒H ‒H ‒F 0.7
  KS21 ‒Br ‒OH ‒H ‒H ‒H ‒OH 13
  KS22 ‒Br ‒OH ‒H ‒H ‒H ‒CH3 3.1
  KS23 ‒Br ‒OH ‒H ‒H ‒H ‒CH2CH3 2.5
  KS24 ‒Br ‒OH ‒H ‒H ‒H ‒p‒PhCl 0.6
  KS27 ‒Br ‒OH ‒H ‒H ‒H ‒Br 0.8