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. Author manuscript; available in PMC: 2017 Aug 8.
Published in final edited form as: Bioorg Med Chem. 2017 Mar 28;25(9):2676–2678. doi: 10.1016/j.bmc.2017.03.044

Table 2. Biological activities and physicochemical properties of series 6 and 7.

graphic file with name nihms877862u2.jpg
GI50b (μM) Propertyc
R1 R2 IC50 (μM)a Mer TK A549 KB KB-vin DU145 MV4-11 Aq Sol (μg/mL) Log P
4a graphic file with name nihms877862t13.jpg OMe 1.08 10.1 11.1 12.6 12.4 4.91 10.4 >5
6a graphic file with name nihms877862t14.jpg CN >30 >31.3 >31.3 >31.3 >31.3 NDd ND ND
6b graphic file with name nihms877862t15.jpg NH2 7.27 15.9 17.4 21.7 18.7 4.42 ND ND
6c graphic file with name nihms877862t16.jpg F 4.17 12.8 13.8 12.3 9.9 5.43 1.54 >5
6d graphic file with name nihms877862t17.jpg OH 1.24 14.8 12.1 13.6 14.3 3.00 3.10 3.95
6e graphic file with name nihms877862t18.jpg COOH 2.90 28.7 25.2 19.8 27.3 7.50 ND ND
4b graphic file with name nihms877862t19.jpg OMe 0.68 15.2 20.3 17.1 18.3 8.75 95.6 2.54
7a graphic file with name nihms877862t20.jpg CN 1.72 3.00 23.7 4.31 18.7 2.79 7.52 2.84
7b graphic file with name nihms877862t21.jpg NH2 >30 17.1 19.7 18.7 20.8 ND ND ND
7c graphic file with name nihms877862t22.jpg F >30 19.3 17.1 24.2 20.6 ND ND ND
7d graphic file with name nihms877862t23.jpg F 7.84 4.3 2.9 2.5 4.2 ND ND ND
7e graphic file with name nihms877862t24.jpg F >30 ND ND ND ND ND ND ND
7f graphic file with name nihms877862t25.jpg NH2 >30 ND ND ND ND ND ND ND
Staurosporinee 0.00081
Paclitaxel (nM)e 4.9 2.6 948 2.6
a

IC50 is concentration that inhibits 50% Mer tyrosine kinase.

b

GI50 is concentration that inhibits 50% human tumor cell growth, and the values were averaged values determined by at least three independent experiments.

c

Active compounds with IC50 < 10 μM and GI50 < 20 μM were measured by the methods in Ref. 19.

d

Not detected.

e

Reference compounds as the positive control in related assays.