TY - JOUR
T1 - Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor
AU - Luo, Zonghua
AU - Liu, Hui
AU - Klein, Robyn S.
AU - Tu, Zhude
N1 - Publisher Copyright:
© 2019 Elsevier Ltd
PY - 2019/8/15
Y1 - 2019/8/15
N2 - Twenty eight new aryloxybenzene analogues were synthesized and their in vitro binding potencies toward S1PR2 were determined using a [32P]S1P competitive binding assay. Out of these new analogues, three compounds, 28c (IC50 = 29.9 ± 3.9 nM), 28e (IC50 = 14.6 ± 1.5 nM), and 28g (IC50 = 38.5 ± 6.3 nM) exhibited high binding potency toward S1PR2 and high selectivity over the other four receptor subtypes (S1PR1, 3, 4, and 5; IC50 > 1000 nM). Each of the three potent compounds 28c, 28e, and 28g contains a fluorine atom that will allow to develop F-18 labeled PET radiotracers for imaging S1PR2.
AB - Twenty eight new aryloxybenzene analogues were synthesized and their in vitro binding potencies toward S1PR2 were determined using a [32P]S1P competitive binding assay. Out of these new analogues, three compounds, 28c (IC50 = 29.9 ± 3.9 nM), 28e (IC50 = 14.6 ± 1.5 nM), and 28g (IC50 = 38.5 ± 6.3 nM) exhibited high binding potency toward S1PR2 and high selectivity over the other four receptor subtypes (S1PR1, 3, 4, and 5; IC50 > 1000 nM). Each of the three potent compounds 28c, 28e, and 28g contains a fluorine atom that will allow to develop F-18 labeled PET radiotracers for imaging S1PR2.
KW - Binding potency
KW - Positron emission tomography
KW - Selectivity
KW - Sphingosine 1-phosphate receptor 2
UR - http://www.scopus.com/inward/record.url?scp=85068234186&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2019.06.047
DO - 10.1016/j.bmc.2019.06.047
M3 - Article
C2 - 31279524
AN - SCOPUS:85068234186
SN - 0968-0896
VL - 27
SP - 3619
EP - 3631
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 16
ER -