Skip to main content
. Author manuscript; available in PMC: 2019 Dec 15.
Published in final edited form as: Clin Cancer Res. 2018 Sep 5;24(24):6509–6522. doi: 10.1158/1078-0432.CCR-18-0982

Table 1:

Structure-activity analysis of compound Hit 1

Structurea Flavonoid –R3 –R5 –R6 –R7 –R3’ –R4’ IC50(μM)b
graphic file with name nihms-1506048-t0006.jpg 5,7,3’,4’-Tetrahydroxyflavone H OH H OH OH OH 1.01
5,3’,4’-Trihydroxyflavone H OH H H OH OH 1.01
5,7,4’-Trihydroxyflavone H OH H OH H OH No effect
7,3’,4’-Trihydroxyflavone H H H OH OH OH No effect
5.7-Dihydroxyflavone H OH H OH H H No effect
3’.4’-Dihydroxyflavone H H H H OH OH No effect
7,3’-Dihydroxyflavone H H H OH OH H No effect
5,4’-Dihydroxyflavone H OH H H H OH 5.48
5,3’-Dihydroxyflavone H OH H H OH H 0.53
7,4’-Dihydroxyflavone H H H OH H OH No effect
5-Hydroxyflavone H OH H H H H >10
3’-Hydroxyflavone H H H H OH H No effect
5,3’-Dihydroxy-6,7,4’-trimethoxyflavone H OH OCH3 OCH3 OH OCH3 4.17
5,7,4’-Trihydroxy-3’-methoxyflavone H OH H OH OCH3 OH No effect
5,7,3’-Trihydroxy-4’-methoxyflavone H OH H OH OH OCH3 1.37
5,7,3’,4’-Tetrahydroxy-3-methoxyflavone OCH3 OH H OH OH OH No effect
5,7,3’,4’-Tetramethoxyflavone H OCH3 H OCH3 OCH3 OCH3 No effect
a

R8, R2’, R5’ and R6’ comprise H in all cases

b

IC50 for inhibition of ELK1-dependent promoter activation by AR. The primary screening assay (ELK1-dependent promoter activation by AR) was used to determine the IC50 values for Hit1 and its various derivatives, using a compound dose range of 1-10μM.