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. Author manuscript; available in PMC: 2015 Jul 15.
Published in final edited form as: J Med Chem. 2011 Aug 17;54(18):6254–6276. doi: 10.1021/jm200570p

Table 3.

In vitro cytotoxicity of 3-amino substituted esters 26 and acids 27 and sodium salt 28

graphic file with name nihms317976u3.jpg
Compd R1 R2 IC50 (μM)
DU145 K562
26a 2, 4, 6-(CH3O)3 CH2 0.1 0.1
26b 3, 4, 5-(CH3O)3 CH2 75 30
26c 2, 4, 6-(CH3O)3 CH2CH2 1.5 1.0
26d 2, 4, 6-(CH3O)3 CH(CH3) 0.75 0.2
26e 2, 4, 6-(CH3O)3 CF2 0.25 0.25
26f 2, 4, 6-(CH3O)3 CH(CF3) 0.25 0.25
26g 2, 4, 6-(CH3O)3 C(CH3)2 2.5 0.80
26h 2, 4, 6-(CH3O)3 CH(C6H5) 0.075 0.03
26i 2, 4, 6-(CH3O)3 CH(4-FC6H4) 0.3 0.8
26j 2, 4, 6-(CH3O)3 CH(4-ClC6H4) 0.4 0.2
26k 2, 4, 6-(CH3O)3 CH(4-BrC6H4) 0.3 0.2
26l 2, 4, 6-(CH3O)3 CH(4-MeOC6H4) 0.25 0.15
27a 2, 4, 6-(CH3O)3 CH2 0.075 0.0075
27b 3, 4, 5-(CH3O)3 CH2 5.0 3.0
27c 2, 4, 6-(CH3O)3 CH2CH2 5.0 5.0
27d 2, 4, 6-(CH3O)3 CH(CH3) 0.025 0.015
27e 2, 4, 6-(CH3O)3 CF2 0.15 0.15
27f 2, 4, 6-(CH3O)3 CH(CF3) 0.02 0.075
27g 2, 4, 6-(CH3O)3 C(CH3)2 0.15 0.0075
27h 2, 4, 6-(CH3O)3 CH(C6H5) 0.02 0.015
27i 2, 4, 6-(CH3O)3 CH(4-FC6H4) 0.15 0.08
27j 2, 4, 6-(CH3O)3 CH(4-ClC6H4) 0.4 0.25
27k 2, 4, 6-(CH3O)3 CH(4-BrC6H4) 0.3 0.2
27l 2, 4, 6-(CH3O)3 CH(4-OMeC6H4) 0.1 0.015
28 ON 01910 Na 0.1 0.015