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. Author manuscript; available in PMC: 2014 Sep 1.
Published in final edited form as: Bioorg Med Chem. 2013 Jun 26;21(17):10.1016/j.bmc.2013.06.046. doi: 10.1016/j.bmc.2013.06.046

Table 1.

Cytotoxicity of compounds 12a–n.

graphic file with name nihms506562t1.jpg
Compd R2 R3 R4 R5 R6 IC50(µM)a
MCF-7 2774 SKOV-3 HL-60 Hep 3B H460 COLO 205 A498 Detroit 551
Un-substituted
12a H H H H H 18.5 >30 >30 >50 >50 >50 >50 42.7 >50
Mono-substituted
12b OCH3 H H H H 27.1 18.8 26.6 10 23.3 >25 18.1 9.8 >25
12c H OCH3 H H H 14.9 15.6 24.6 >10 >10 >10 39.6 >50 >10
12d H H OCH3 H H >30 >30 26.8 >20 >20 >20 >50 >25 >20
Di-substituted
12e OCH3 H OCH3 H H 6.0 0.4 0.4 0.4 1.0 0.9 7.4 48 >25
12f OCH3 H H OCH3 H 3.7 6.5 20 3.5 10 10 6.1 28.9 >100
12g OCH3 H H H OCH3 29.8 >30 >30 >100 >100 >100 >50 >50 >100
12h H OCH3 OCH3 H H 14.3 6.6 6.4 4.1 14.6 14.4 16.8 25.6 23.6
12i H OCH3 H OCH3 >30 8.3 >30 2.9 >10 >10 >50 11.7 >10
Tri-substituted
12j OCH3 H OCH3 H OCH3 21 >30 >30 75 >100 67.6 37.4 >50 >100
12k H OCH3 OCH3 OCH3 H 4.5 2.1 0.93 2.3 5.0 7.6 >50 >50 >25
Fluoro-substituted
121 F H H H H >30 26.4 >30 >100 >100 >100 >50 >50 >100
12m H H H H >30 24.5 >30 >20 >20 >20 >50 >50 >20
12n H H F H H >30 17.6 >30 >60 >20 >20 >50 >50 >20
Etoposide 5.48 1.0
5-FU 22.3 26.7

Human tumor cells were treated with different concentrations of samples for 48 h (n = 3 independent experiments).

a

Data are presented as IC50 (µM, the concentration of 50% proliferation-inhibitory effect).