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. Author manuscript; available in PMC: 2017 Jul 1.
Published in final edited form as: Bioorg Med Chem. 2016 May 17;24(13):3083–3092. doi: 10.1016/j.bmc.2016.05.025

Table 1.

Biological activities and physicochemical properties of series 4 and 5

graphic file with name nihms790823t1.jpg
R1 R3 IC50 (µM)a
Mer TK		 GI50 (µM)b Propertiesc
A549 KB KB-vin DU145 MV4-11 Aq. Sol.
(µ g/mL)		 Log P
4a graphic file with name nihms790823t2.jpg H 1.08 10.1 11.1 12.6 12.4 4.91 10.4 >5
5a graphic file with name nihms790823t3.jpg Me 1.14 9.4 11.7 10.1 10.2 2.70 1.11 >5
4b graphic file with name nihms790823t4.jpg H 0.68 15.2 20.3 17.1 18.3 8.75 95.6 2.54
5b graphic file with name nihms790823t5.jpg Me 2.01 13.0 24.8 30.8 30.2 70.1 ND ND
4c graphic file with name nihms790823t6.jpg H 3.43 3.53 5.33 5.09 4.08 5.88 4.36 >5
5c graphic file with name nihms790823t7.jpg Me 1.84 12.4 13.7 12.4 13.0 2.33e 3.43 >5
4d graphic file with name nihms790823t8.jpg H 2.25 16.1 14.8 17.5 14.3 3.07 6.61 3.21
5d graphic file with name nihms790823t9.jpg Me 10.2 19.9 18.7 22.9 24.3 ND ND ND
4e graphic file with name nihms790823t10.jpg H 2.06 20.1 21.0 15.3 20.1 ND ND ND
5e graphic file with name nihms790823t11.jpg Me >30 NDd ND ND ND ND ND ND
4f graphic file with name nihms790823t12.jpg H 3.56 13.0 13.3 13.4 13.0 <13.4 ND ND
5g graphic file with name nihms790823t13.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 Reference 19;

d

not detected;

e

tested in human chronic myelogenous leukemia (K526) cells;

f

reference compounds as the passitive control in related assays.