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. Author manuscript; available in PMC: 2019 Jul 26.
Published in final edited form as: J Med Chem. 2018 Jul 13;61(14):6163–6177. doi: 10.1021/acs.jmedchem.8b00583

Table 2:

Substituents on the Thiazolium Ring are Important for Bioactivity

graphic file with name nihms-982610-t0010.jpg

Compd R3 MCF-7
IC50/μM
MDA-MB-231
IC50/μM
MEF
IC50/μM

JG-98 graphic file with name nihms-982610-t0011.jpg 0.71 ± 0.22 0.39 ± 0.03 4.2 ± 1
22 graphic file with name nihms-982610-t0012.jpg 0.19 ± 0.01 0.18 ± 0.02 0.70 ± 0.03
33 graphic file with name nihms-982610-t0013.jpg 0.16 ± 0.01 0.16 ± 0.01 1.4 ± 0.1
34 graphic file with name nihms-982610-t0014.jpg 1.5 ± 0.1 1.6 ± 0.2 1.7 ± 0.1
35 graphic file with name nihms-982610-t0015.jpg >5 7.2 ± 0.8 > 5
36 graphic file with name nihms-982610-t0016.jpg 0.21 ± 0.01 0.12 ± 0.02 5.5 ± 0.5
37 graphic file with name nihms-982610-t0017.jpg 1.5 ± 0.1 0.97 ± 0.10 2.0 ± 0.2
38 graphic file with name nihms-982610-t0018.jpg 0.81 ± 0.09 0.13 ± 0.01 2.7 ± 0.1
39 graphic file with name nihms-982610-t0019.jpg 0.73 ± 0.06 0.11 ± 0.01 4.4 ± 0.3
40 graphic file with name nihms-982610-t0020.jpg 0.16 ± 0.02 0.22 ± 0.02 3.2 ± 0.3
41 graphic file with name nihms-982610-t0021.jpg 0.52 ± 0.09 0.20 ± 0.02 1.3 ± 0.1
42(JG-231) graphic file with name nihms-982610-t0022.jpg 0.12 ± 0.01 0.25 ± 0.02 2.5 ± 0.1
43 graphic file with name nihms-982610-t0023.jpg 0.098 ± 0.008 0.080 ± 0.008 4.2 ± 0.4
44 graphic file with name nihms-982610-t0024.jpg 0.96 ± 0.08 0.74 ± 0.07 4.9 ± 0.3
45 graphic file with name nihms-982610-t0025.jpg >5 2.3 ± 0.3 8.9 ± 0.8
46 graphic file with name nihms-982610-t0026.jpg >5 >20 4.2 ± 0.6
47 graphic file with name nihms-982610-t0027.jpg >5 10 ± 2 7.6 ± 0.3