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. 2017 Mar 1;8(4):407–412. doi: 10.1021/acsmedchemlett.6b00489

Table 2. SAR Study of Compounds 21–33.

graphic file with name ml-2016-00489w_0006.jpg

No. R4 EC50(nM)a
21 2-Cl 1143 ± 235
22 3-Cl 257 ± 37
23 4-Cl 66 ± 4.2
24 3-OH 1821 ± 371
25 3-OMe 57 ± 1.7
26 3-OEt 110 ± 25
27 3-OPr 69 ± 9.7
28 4-OMe 94 ± 9.6
29 3-ethynyl 4477 ± 1040
30 4-ethynyl 817 ± 189
31 3-cyano 4060 ± 477
32 4-cyano 3489 ± 184
33b 3,4-dimethoxy 25 ± 0.57
a

EC50: cellular apoptosis inhibition in the U2OS_Bim cell line.

b

Compound A.