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. Author manuscript; available in PMC: 2014 Jun 1.
Published in final edited form as: Eur J Med Chem. 2013 Apr 8;64:512–528. doi: 10.1016/j.ejmech.2013.03.066

Table 5.

Activity of compounds 6a–w (Scheme 1) in HL-60 cells expressing human FPR1, FPR2,or FPR3

graphic file with name nihms482194t1.jpg
Compd. R OCH3 R1 Ca2+ Mobilization EC50 (µM) and Efficacy (%) a
FPR1 FPR2 FPR3 W.T.b
A16 CH3 m 3,4-methylenedioxy 2.3 (50) N.A. N.A. N.A.
B16 CH3 p Br (p) N.A. 2.4 N.A. N.A.
C16 CH3 m I (p) 2.8 (90) 6.8 (40) 13.0 (30) N.A.
D16 CH3 m Br (p) 3.4 (75) 3.8 (70) N.A. N.A.
6a H m Br (p) 6.1 (125) 7.7 (60) 14.6 (25) N.A.
6b CH2CH3 m I (p) 4.2 (70) 5.5 (65) N.A. N.A.
6c CH(CH3)2 m Br (p) 4.5 (135) 7.2 (90) 17.4 (30) N.A.
6d C6H11 m Br (p) 10.8 (80) N.A. N.A. N.A.
6e C6H5 m Br (p) 9.0 (110) 4.3 (25) N.A. N.A.
6f C6H5 m 3,4-methylenedioxy N.A. N.A. N.A. N.A.
6g C6H5 m F (p) N.A. N.A. N.A. N.A.
6h 2-thienyl p Br (p) N.A. N.A. N.A. N.A.
6i 2-thienyl m 3,4-methylenedioxy N.A. N.A. N.A. N.A.
6j 2-thienyl m F (p) N.A. N.A. N.A. N.A.
6k C6H4-OCH3 (p) p Br (p) N.A. N.A. N.A. N.A.
6l C6H4-OCH3 (p) m 3,4-methylenedioxy N.A. N.A. N.A. N.A.
6m C6H4-OCH3 (p) m F (p) N.A. N.A. N.A. N.A.
6n C6H4-Cl (p) p Br (p) N.A. N.A. N.A. N.A.
6o C6H4-Cl (p) m 3,4-methylenedioxy N.A. N.A. N.A. N.A.
6p C6H4-Cl (p) m F (p) N.A. N.A. N.A. N.A.
6q C6H4-CH3 (p) p Br (p) N.A. N.A. N.A. N.A.
6r C6H4-CH3 (p) m 3,4-methylenedioxy N.A. N.A. N.A. N.A.
6s C6H4-CH3 (p) m F (p) N.A. N.A. N.A. N.A.
6t C6H4-F (p) p Br (p) N.A. N.A. N.A. N.A.
6u C6H4-F (p) m 3,4-methylenedioxy N.A. N.A. N.A. N.A.
6v C6H4-F (p) m F (p) N.A. N.A. N.A. N.A.
6w CH2-C6H5 p Br (p) N.A. N.A. N.A. N.A.
a

N.A., no activity (no response was observed during first 2 min after addition of compounds under investigation) considering the limits of efficacy > 20 % and EC50 < 50 µM.

b

W.T., wild-type nontransfected HL-60 cells. The EC50 values are presented as the average mean of three independent experiments, in which EC50 values were determined by nonlinear regression analysis of the dose-response curves (5–6 points) generated using GraphPad Prism 5 with 95% confidential interval (p< 0.05). Efficacy (in brackets) is expressed as % of the response induced by 5 nM fMLF (FPR1) or 5 nM WKYMVm (FPR2 and FPR3).