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Rhodamine Cyclen-based Fluorescent Chemosensor for the Detection of Cd^(2+)
Soyoung Shim,태진성 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.8
A chemosensor based on a rhodamine-hydroxamate platform containing a pyridine and a cyclen binding units has been developed for the detection of Cd^(2+) in aqueous solutions. The probe responds selectively toward Cd^(2+)over other biologically relevant metal ions. The fluorescent probe shows 1:1 binding stoichiometry and the detection limit for Cd^(2+) in water proved to be as low as 25 nM.
Synthesis of N-Alkyl-Carbazole Derivatives as 5-HT7R Antagonists
김영재,염미영,이소연,태진성,김학중,임혜원,성지혜,최경일,민선준,추현아 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.9
We designed and synthesized a series of N-alkyl-carbazoles with different alkyl chains and amine moieties, and biological evaluation was performed to discover novel 5-HT7R antagonists. Among 27 synthesized compounds, 20, 21, 23, and 24 showed excellent binding affinities to 5-HT7R (Ki = 65, 64, 55, and 31 nM, respectively), and good selectivity profiles over other serotonin receptors. In functional assays, those compounds showed weak antagonistic activities against 5-HT7R. In particular, the compound 24, 2-(4-(5-(9H-carbazol-9-yl)pentyl)piperazin-1-yl)phenol, could be considered as a potent and selective 5-HT7R ligand with weak antagonistic effect. From the molecular docking study, the aromatic hydroxyl group in 24 was shown to play an important role in binding to 5-HT7R through a hydrogen bonding interaction with Asp142 in the ligand binding pocket of 5-HT7R.
심영선,이예용,왕현정,태진성,박종현,추현아,임혜원,남길수 대한화학회 2023 Bulletin of the Korean Chemical Society Vol.44 No.7
A novel series of 4-arylthio- or 4-arylsulfonyl-substituted 2-amino-5,6,7,8- tetrahydroquiazolines was synthesized and evaluated for serotonin receptor subtype 6 (5-HT6R) antagonistic effects in vitro. The structure activity relationships (SAR) of this series were discussed on the basis of in vitro activity. Among the derivatives synthesized in the present study, the lead compound, 7a, having sulfonyl functionality at the 4-position and N-methylpiperazine at the 2-position of the core structure showed the most potent 5-HT6 receptor inhibitory activity in vitro and good metabolic stability without CYP liability.
Byung Sun Park,유경호,한동근,태진성,이소하,Ibrahim M. El-deeb 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.11
A series of new 4-(pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles (6a-k & 7a-l) has been rationally designed based on the structure of the lead compound KIST301080, a selective ROS receptor tyrosine kinase inhibitor, in order to study the activity of ROS of this new class of inhibitors. The compounds were synthesized and screened against ROS kinase, where compound 6h showed moderate inhibitory activity with an IC50 value of 6.25 μM. The study emphasized the importance of the acetonitrile group at the pyrazole ring and also the importance of having a hydrogen bond donor on the distal phenyl ring linked to the pyridine moiety.
Mohammad M. Al-Sanea,박병선,Ahmed Z. Abdelazem,Khalid B. Selim,유경호,심태보,태진성,이소하 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.1
A series of rationally designed ROS1 tyrosine kinase inhibitors 6a–9b with bipyridinyl pyrazole scaffold was synthesized and screened. The scaffold itself has showed an exclusive selectivity profile over ROS1 closely related kinases,ALKand c-Met. The aim of this study was to further explore the structure–activity relationships (SAR) of the bipyridinyl pyrazole core structure, and to improve its ROS1 inhibitory potency. The rational of this study was to explore the nature of the proposed binding site for the pyrazoleNHsubstituents. Careful selections of pyrazoleNHsubstituent groups along with their regioisomers were considered. The compounds exhibited high degree of potency, IC50 values of 21–159 nM. A detailed SAR of bipyridinyl pyrazole scaffold has been finally well established and the virtual screening strategy, through molecular docking, has been performed for this type of ROS1 kinase inhibitors and the docked poses along with the activity data have gone in consistent with SAR specifications.