• Title/Summary/Keyword: Fluoro

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Synthesis of 1N-aryl-2-methyl-3-ethoxycarbonyl-pyridino [2,3-f]indole-4,9-dione derivatives (II) (1N-아릴-2-메틸-3-에톡시카르보닐-피리디노 [2,3-f]인돌-4,9-디온 유도체의 합성 (II))

  • Suh, Myung-Eun;Park, Hee-Kyung
    • YAKHAK HOEJI
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    • v.41 no.5
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    • pp.582-587
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    • 1997
  • The 6.7-dichloroquinoline-5,8-dione (I) was reacted with ethyl acetoacetate in the presence of sodium ethoxide to yield 6-(${\alpha}$-acetyl-${\alpha}$-ethoxycarbonyl methyl)-7-chloro-qui noline-5,8-dione(II). When this compound II was reacted with some arylamine (phenyl, p-toluyl, p-fluorophenyl, p-chlorophenyl. p-bromophenyl, p-iodophenyl, p-trifluoromethylphenyl, p-dimethylaminophenyl,indanyl), 1N-aryl-2-methyl-3-ethoxycarbonyl pyridino[2,3-f]-indole-4.9-dione(IIIa-I) were obtained via intramolecular cyclization.

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The Determination of Enoxacin with p-Quinone Derivatives (파라퀴논 유도체와의 전하이동착물 형성을 이용한 에녹사신 정량)

  • 이지연;김동오;남수자;정문모;허문회;안문규
    • YAKHAK HOEJI
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    • v.43 no.4
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    • pp.437-441
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    • 1999
  • Enoxacin[1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-\piperazinyl)-1,8-naphthyridine-3-carboxylic acid, ENX] is a new quinolone antibacterial agent. The method is based on the highly colored charge-transfer complex formation of this drug as a $\pi$-electron donor with 7,7,8,8-tetracyanoquinodimethane(TCNQ) or chloranil(CL) as $\pi$-acceptors. The colored products were measured spectrophotometrically at 842 nm and 552 nm for TCNQ and CL, respectively. The different experimental conditions are optimized. The linearities for TCNQ and CL were $1.6{\;}\mu\textrm{g}/mL~32{\;}\mu\textrm{g}/mL$ and $6.4{\;}\mu\textrm{g}/mL~160{\;}\mu\textrm{g}/mL$, respectively and colors were produced in non-aqueous media. This report describes a simple and ra\pid method for the analysis of enoxacin.

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Synthesis of (-)-Neplanocin A Analogues as Potential Antiviral Agents

  • Shin, Dae-Hong;Lee, Hyuk-Woo;Park, Sung-Soo;Kim, Joong-Hyup;Jeong, Lak-Shin;Chun, Moon-Woo
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.302-309
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    • 2000
  • Based on (-)-neplanocin A with the 5'-hydroxyl substituted with fluoro, azido, or amino group, the corresponding xylo- and arabino derivatives were synthesized from D-ribose using the Mit-sunobu reaction as a key step. None of the final nucleosides did show either significant antiviral activities or cytotoxicities.

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Seismic Responses of Seismically Isolated Nuclear Power Plant Structure Considering Post-Yield Stiffness of EQS Bearing (EQS 면진장치의 항복 후 강성을 고려한 면진 원전구조물의 지진응답)

  • Kim, Byeong-Su;Song, Jong-Keol
    • Journal of the Earthquake Engineering Society of Korea
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    • v.20 no.5
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    • pp.319-329
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    • 2016
  • The Eradi Quake System (EQS) is a seismic isolation bearing system designed to minimize forces and displacements experienced by structures subjected to ground motion. The EQS dissipates seismic energy through friction of Poly Tetra Fluoro Ethylene (PTFE) disk pad. In general, a force-displacement relationship of EQS has post yield stiffness hardening during large inelastic displacement. In this study, seismic responses of seismically isolated nuclear power plant (NPP) subjected to design basis earthquake (DBE) and beyond design basis earthquakes (150% DBE and 167% DBE) are compared considering the post yield stiffness hardening effect of EQS. From the results, it can be observed that if the post-yield stiffness hardening effect of EQS is increased, the displacement response of EQS is reduced, and the acceleration and shear responses of containment structures of NPP is increased.

Effects of Herbal Medicines on Monoamine Oxidase Activity (수종의 천연물이 Monoamine Oxidase 활성에 미치는 영향 (제3보) : 황련, 계피, 지실의 활성 저해작용)

  • Lee, Sang Seon;Kim, Young Ho;Lee, Myung Koo
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.139-142
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    • 1998
  • The effects of MeOH extracts from 28 herbal medicines on monoamine oxidase (MAO) activity were investigated. MAO was purified from mouse brain and its activity was determined by fluoro-photometry using kynuramine as a substrate. Three MeOH extracts, Coptis japonica, Cinnamomum cassia and Poncirus trifoliate from the herbal medicines showed a strong inhibitory effect with less than $100\;{\mu}g/ml$ in their inhibitory amounts of $50\%$ ($IC_{50}$ values) on MAO activity. Four MeOH extracts including Evodia officinalis exhibited a mild inhibition of MAO activity with $100-200\;{\mu}g/ml$ in their $IC_{50}$ values.

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Synthesis of New Pyrimidinylaminobenzene Derivatives and Their Antiproliferative Activities against Melanoma Cell Line

  • Kim, Hee Jin;Oh, Chang-Hyun;Yoo, Kyung Ho
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2311-2316
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    • 2013
  • A series of new diarylamide and diarylurea derivatives possessing pyrimidinylaminobenzene scaffold was synthesized. Their in vitro antiproliferative activities were tested against A375P human melanoma cell line. Among them, compounds 1a-c, k and 2b-d, f, g, j, l showed superior potencies against A375P human melanoma cell line to Sorafenib. In particular, compound 2f possessing 3-fluoro-5-trifluoromethyl moiety exhibited the highest potency with $IC_{50}$ value in nanomolar scale.

Primary Intracranial Malignant Melanoma with Extracranial Metastasis

  • Hirota, Kengo;Yoshimura, Chika;Kubo, Osami;Kasuya, Hidetoshi
    • Journal of Korean Neurosurgical Society
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    • v.60 no.1
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    • pp.98-101
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    • 2017
  • We report a case of primary intracranial malignant melanoma (PIMM) with extracranial metastases. The patient was an 82-year-old woman diagnosed with PIMM under the left cerebellar tentorium. We performed a tumor resection followed by gamma knife surgery. An magnetic resonance imaging at 11 months after surgery showed a local intracranial recurrence. At 12 months, vertebral metastasis was suspected, and 2-[fluorine-18]-fluoro-2-deoxy-D-glucose positron emission tomography/computed tomography (FDG-PET/CT) showed multiple extracranial metastases. She died at 13 months after surgery. Although extracranial metastases of PIMM are extremely rare, we should carefully follow up extracranial metastases together with intracranial ones, especially by FDG-PET/CT, even at an early asymptomatic stage.

Lobular Breast Carcinoma Metastasis to the Thyroid Gland: Case Report and Literature Review

  • Bourcier, Kevin;Fermeaux, Veronique;Leobon, Sophie;Deluche, Elise
    • Journal of Breast Cancer
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    • v.21 no.4
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    • pp.463-467
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    • 2018
  • Metastasis from primary cancer to the thyroid is uncommon in breast cancer. Here we present a case of lobular breast carcinoma that metastasized to the thyroid. A 54-year-old woman without symptoms was admitted to our institution for staging of the lymph node above the left clavicle. An $^{18}F$-fluoro-deoxy-D-glucose positron emission tomography scan was performed for staging, and low uptakes were observed in the left supraclavicular and cervical lymph nodes. High uptake was seen in the posterior and lower left lobe of the thyroid. Histologic findings indicated lobular breast carcinoma (positive GATA3, loss of E-cadherin expression) metastatic to the thyroid with a luminal profile. Immunohistochemical analysis was negative for primary thyroid or parathyroid carcinoma. To our knowledge, this is the first report of a patient presenting a metastatic invasive lobular carcinoma in the thyroid and lymph nodes without a prior diagnosis of breast cancer.

DESIGN AND SYNTHESIS OF A3 ADENOSINE RECEPTOR LlGANDS. 3′-FLUORO ANALOGUES OF CI- IB-MECA

  • Lim, Moo-Hong;Kim, Hea-Ok;Moon, Hyung-Ayong;Chun, Moon-Woo;Jeong, Lak-Shin
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.364.1-364.1
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    • 2002
  • 2-Chloro-N6-(3-iodobenzyl)-adenosine-5'-methylcarboxamide (2-CI-IB-MECA) has been recognized to be one of the most selective agonists (Ki = 1.0 nM) for rat adenosine A3 receptor. On the basis of the high binding affinity of 2-CI-IB-MECA to adenosine A3 receptor. it was interesting to find out whether 2'- and/or 3'-hydroxyl group of 2-CI-IB-MECA is essential for the binding affinity to the receptor. (omitted)

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DESIGN AND SYNTHESIS OF A3 ADENOSINE RECEPTOR LlGANDS, 2′-FLUORO ANALOGUES OF CI- IB-MECA

  • Park, Jae-Gyu;Kim, Hea-Ok;Moon, Hyung-Ryong;Jeong, Lak-Shin
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.365.1-365.1
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    • 2002
  • Since adenosine A3 receptor has been cloned from rat brain. a number of compounds have been synthesized and evaluated for the binding affinity to this receptor. Among these. 2-chloro-N6-(3-iodobenzyl)-adenosine-5'-methylcarboxamide (2-CI-IB-MECA) has been found to be one of the most selective agonists (Ki = 1.0 nM) for rat adenosine A3 receptor. On the basis of the high binding affinity of 2-CI-IB-MECA to adenosine A3 receptor. it was interesting to find out whether 2'-hydroxyl group of 2-CI-IB-MECA is essential for the binding affnity to the receptor. (omitted)

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