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. Author manuscript; available in PMC: 2016 Apr 18.
Published in final edited form as: J Med Chem. 2015 Sep 17;58(19):7734–7748. doi: 10.1021/acs.jmedchem.5b00686

Table 1.

Compounds, and their side chains, inhibitory activities against U251MG, MDA-MB-231, NIH3T3 cell growth, and Stat3-inhibitory activity inside and outside of cells.

graphic file with name nihms775634u2.jpg
Cpd R R′ R″ Inhibition of cell growth Inhibition against Stat3 signaling
U251MG MDA-MB-231 SF295 NIH 3T3 pYStat3 (cellular) DNA binding activity (cellular) Stat3/DNA complexation (cell-free)
6 H graphic file with name nihms775634t1.jpg graphic file with name nihms775634t2.jpg +++ +++ ++ +++ +++ +++ ++
7 H graphic file with name nihms775634t3.jpg graphic file with name nihms775634t2.jpg ++ + +/− + ++ nd ++
8 H graphic file with name nihms775634t1.jpg H +/− +/− +/− − − nd −
9 CH3 graphic file with name nihms775634t3.jpg graphic file with name nihms775634t2.jpg +/− − − − − − −
10 CH3 graphic file with name nihms775634t1.jpg graphic file with name nihms775634t2.jpg ++ + − +/− ++ +++ +
11 H H graphic file with name nihms775634t2.jpg +/− +/− − − − + +++
14 H H H − − +/− − − nd −
15 CH3 H H +/− +/− − − nd nd nd
17 CH3 graphic file with name nihms775634t1.jpg H +/− − +/− − nd nd nd
18 H graphic file with name nihms775634t3.jpg H +/− − − − − nd −
19 H graphic file with name nihms775634t4.jpg H +/− − − − − nd −
20 H graphic file with name nihms775634t4.jpg graphic file with name nihms775634t2.jpg ++ +/− +/− +/− ++ nd +++
21 H graphic file with name nihms775634t5.jpg H − − − − − nd −
22 H H graphic file with name nihms775634t1.jpg ++ +/− +/− +/− +++ +++ +++
28 CH3 graphic file with name nihms775634t3.jpg H +/− − +/− − − nd −

Bold, most active agents; nd, not determined; +++ strongly active; ++ very active; + active; +/− moderately active or less active; − no activity; activities are measured at 5 μM; cpd, compound