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전문국,김정규,이덕형 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.9
The coupling of 7-aryl-3,4-dihydro-4-oxothieno[3,2-d]pyrimidine-2-carboxylic acid with a primary alkylamine-loaded acid-sensitive methoxy benzaldehyde (AMEBA) resin, a benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP)-mediated amination reaction, and cleavage from the solid support yielded N-alkyl-4-(alkylamino)-7-arylthieno[3,2-d]pyrimidine-2-carboxamide derivatives. The progress of the reactions on solid phase was monitored through attenuated total reflectance-FTIR spectroscopy and was compared with representative solution-phase surrogates. Additionally, N-acylation (acid chloride, InF3, CH3CN, room temperature) and cyclization (DBN, 1,4-dioxane, 80°C) of a 3-amino-4-(4-t-butoxycarbonylphenyl)thiophene-2-carboxamide intermediate under previously unreported conditions provided 2-substituted thieno[3,2-d]pyrimidin-4(3H)-one derivatives, which were subsequently converted to 2-substituted 4-alkylamino-7-[4-(alkylaminocarbonyl)phenyl]thieno[3,2-d]pyrimidine derivatives through a reaction sequence consisting of a BOP-mediated amination reaction, t-butyl deprotection, and amide formation.
전문국,이수진,손성욱 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.8
Tetrasubstituted thieno[3,2-b]pyridin-5(4H)-one derivatives were selected as a highly functionalized heterocyclic scaffold for a multisite-specific tagging process utilizing a previously devised fluorous fluorescent tag system. A suitable synthetic method was established for the 7-alkoxy-2,4,6-trisubstituted-thieno[3,2-b]pyridin-5(4H)-one derivatives, and incorporating t-butoxycarbonyl-functionalized building blocks into the reaction sequence produced precursors that could be used in the tagging process. Fluorous solid-phase extraction facilitated the purification of the tagged target compounds after a series of reactions, including t-Bu deprotection/N-hydroxysuccinimidyl ester formation/amidation.
Discovery of 1,2-Naphthoquinone Derivatives as Potent p53-MDM2 Interaction Inhibitors
정명은,고아름,유다빈,채종학,전문국,임병호,최길돈 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.12
Discovery of 1,2-naphthoquinone analogues as potent p53-MDM2 interaction inhibitors.
안서현,김은혜,이채미,남윤채,이주연,송진숙,김성환,전문국 대한화학회 2023 Bulletin of the Korean Chemical Society Vol.44 No.11
A central nervous system (CNS)-oriented compound collection was screened to find hit compounds for human glioblastoma T98G cell growth inhibition. A series of quinoxaline-based derivatives were identified as hit compounds having one- to two-digit micromolar GI50 values. Anti-glioblastoma activity was improved in structure–activity relationship studies varying the substituents on the quinoxaline ring system, resulting in the discovery of four compounds exhibiting sub-micromolar GI50 values. The potentials of the four compounds to induce apoptosis were confirmed by annexin V staining assay. The development potential of the four compounds as CNS drug leads was evaluated by in vitro MDR-MDCK cell permeability and in vivo brain disposition in mice. The mouse pharmacokinetic and kinome profiling studies for compound 10g, which showed high brain-penetrating ability, revealed that the compound is orally bioavailable and inhibits the kinase activities of anaplastic lymphoma kinase (ALK) and Erb-B2 receptor tyrosine kinase (ERBB3).
Novel Indazole-based MKK7–TIPRL Interaction Inhibitors as TRAIL Sensitizers
구수진,정명은,윤지용,윤상은,이정주,LEEKWANGHO,최길돈,김남순,전문국 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.10
This work describes the process by which a metabolically unstable TRT-0002 compound exhibiting Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-sensitizing activity for Huh7 cells at a high working concentration (40??M) is converted to more potent and metabolically improved analogues by modifying the 5-amino group and the 1-aryl moiety in the 1H-indazole skeleton. The efforts enabled us to identify 5-sulfonamido derivatives, TRT-0029 and TRT-0173 compounds, working at lower concentrations (10 and 20??M, respectively) and with improved metabolic stabilities. As reported previously by us, co-treating cultured Huh7 cells with either TRT-0029 or TRT-0173 and TRAIL resulted in TRAIL-induced apoptosis due to the inhibition of the MKK7?TOR signaling pathway regulator-like (TIPRL) interaction and subsequent phosphorylation of MKK7 and JNK. In addition, the injection of TRT-0029 or TRT-0173 compound suppressed tumor growth in combination with TRAIL in an in vivo hepatocellular carcinoma (HCC) mouse xenograft model. TRT-0029 and TRT-0173 compounds and the relevant structure?activity relationship can provide an insight into further study on optimization of potency and metabolic stability.