Skip to main content
. 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 2.

Biological activities and physicochemical properties of series 6 and 7

graphic file with name nihms790823t14.jpg
R1 R2 IC50 (µM)a
Mer TK		 GI50 (µM)b Propertyc
A549 KB KB-vin DU145 MV4-11 Aq. Sol.
(µ g/mL)		 Log P
4a graphic file with name nihms790823t15.jpg OMe 1.08 10.1 11.1 12.6 12.4 4.91 10.4 >5
6a graphic file with name nihms790823t16.jpg CN >30 >31.3 >31.3 >31.3 >31.3 NDd ND ND
6b graphic file with name nihms790823t17.jpg NH2 7.27 15.9 17.4 21.7 18.7 4.42 ND ND
6c graphic file with name nihms790823t18.jpg F 4.17 12.8 13.8 12.3 9.9 5.43 1.54 >5
6d graphic file with name nihms790823t19.jpg OH 1.24 14.8 12.1 13.6 14.3 3.00 3.10 3.95
6e graphic file with name nihms790823t20.jpg COOH 2.90 28.7 25.2 19.8 27.3 7.50 ND ND
4b graphic file with name nihms790823t21.jpg OMe 0.68 15.2 20.3 17.1 18.3 8.75 95.6 2.54
7a graphic file with name nihms790823t22.jpg CN 1.72 3.00 23.7 4.31 18.7 2.79 7.52 2.84
7b graphic file with name nihms790823t23.jpg NH2 >30 17.1 19.7 18.7 20.8 ND ND ND
7c graphic file with name nihms790823t24.jpg F >30 19.3 17.1 24.2 20.6 ND ND ND
7d graphic file with name nihms790823t25.jpg F 7.84 4.3 2.9 2.5 4.2 ND ND ND
7e graphic file with name nihms790823t26.jpg F >30 ND ND ND ND ND ND ND
7f graphic file with name nihms790823t27.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;

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 Reference 19;

d

not detected;

e

reference compounds as the passitive control in related assays.