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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 1. Biological activities and physicochemical properties of series 4 and 5.

graphic file with name nihms877862u1.jpg
GI50 (μM)b Propertiesc
R1 R3 IC50 (μM)a Mer TK A549 KB KB-vin DU145 MV4-11 Aq Sol (μg/mL) Log P
4a graphic file with name nihms877862t1.jpg H 1.08 10.1 11.1 12.6 12.4 4.91 10.4 >5
5a graphic file with name nihms877862t2.jpg Me 1.14 9.4 11.7 10.1 10.2 2.70 1.11 >5
4b graphic file with name nihms877862t3.jpg H 0.68 15.2 20.3 17.1 18.3 8.75 95.6 2.54
5b graphic file with name nihms877862t4.jpg Me 2.01 13.0 24.8 30.8 30.2 70.1 ND ND
4c graphic file with name nihms877862t5.jpg H 3.43 3.53 5.33 5.09 4.08 5.88 4.36 >5
5c graphic file with name nihms877862t6.jpg Me 1.84 12.4 13.7 12.4 13.0 2.33e 3.43 >5
4d graphic file with name nihms877862t7.jpg H 2.25 16.1 14.8 17.5 14.3 3.07 6.61 3.21
5d graphic file with name nihms877862t8.jpg Me 10.2 19.9 18.7 22.9 24.3 ND ND ND
4e graphic file with name nihms877862t9.jpg H 2.06 20.1 21.0 15.3 20.1 ND ND ND
5e graphic file with name nihms877862t10.jpg Me >30 NDd ND ND ND ND ND ND
4f graphic file with name nihms877862t11.jpg H 3.56 13.0 13.3 13.4 13.0 <13.4 ND ND
5g graphic file with name nihms877862t12.jpg Me >30 ND ND ND ND ND ND ND
Staurosporinef 0.00081
Paclitaxel (nM)f 4.9 2.6 948 2.6 ND
a

The concentration that inhibits 50% Mer tyrosine kinase.

b

The concentration inhibits 50% human tumor cell growth, 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

Tested in human chronic myelogenous leukemia (K526) cells.

f

Reference compounds as the positive control in related assays.