Syntheses and bioactivities of songorine derivatives as novel G protein-coupled receptor antagonists
J Wang, C Bian, Y Wang, Q Shen, B Bao, J Fan… - Bioorganic & Medicinal …, 2019 - Elsevier
J Wang, C Bian, Y Wang, Q Shen, B Bao, J Fan, A Zuo, W Wu, R Guo
Bioorganic & Medicinal Chemistry, 2019•ElsevierSongorine isolated from Aconitum brachypodum Diels possesses prominent activity of
inhibiting G protein-coupled receptors (GPCRs) in the early screening process. In this paper,
a series of Songorine derivatives were synthesized and their inhibitory activities on GPCRs
were also evaluated by using the Double Antibody Sandwich ELISA (DAS-ELISA) in vitro.
Among them, three derivatives (3a, 4, 7) exhibited significant inhibitory activity against
GPCRs with IC 50 values of 0.08–0.29 nM. Moreover, the structure-activity relationships …
inhibiting G protein-coupled receptors (GPCRs) in the early screening process. In this paper,
a series of Songorine derivatives were synthesized and their inhibitory activities on GPCRs
were also evaluated by using the Double Antibody Sandwich ELISA (DAS-ELISA) in vitro.
Among them, three derivatives (3a, 4, 7) exhibited significant inhibitory activity against
GPCRs with IC 50 values of 0.08–0.29 nM. Moreover, the structure-activity relationships …
Abstract
Songorine isolated from Aconitum brachypodum Diels possesses prominent activity of inhibiting G protein-coupled receptors (GPCRs) in the early screening process. In this paper, a series of Songorine derivatives were synthesized and their inhibitory activities on GPCRs were also evaluated by using the Double Antibody Sandwich ELISA (DAS-ELISA) in vitro. Among them, three derivatives (3a, 4, 7) exhibited significant inhibitory activity against GPCRs with IC50 values of 0.08–0.29 nM. Moreover, the structure-activity relationships (SARs) of songorine derivatives were discussed in detail. They have great potentials as novel GPCRs antagonists in the future.
Elsevier
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