• 약학회지
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• 제40권6호
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• pp.697-704
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• 1996

Quinolone derivatives, SJ5b (ethyl 5,12-dihydro-5-dihydro-5-oxobenzoxazolo[3,2-a]quinoline-6-carboxylate) and SQ7b (3-fluoro-2-(4-methylpiperazin-1-yl)-5.12-dihydro-5-oxobenzoxa zolo[3,2-a]quinoloine carboxylic acid) showed in vitro cytotoxicities against various tumor cell lines. SJ5b and SQ7b completely inhibited the DNA relaxation activities of human placental topoisomerase II at the concentration of 15.63 and 1.95 ${\mu}$g/ml, respectively. However, unlike etoposide which stabilize the topoisomerase II-DNA complex, SQ7b did not cause topoisomerase II-mediated DNA cleavage and SJ5b weakly stabilized the topoisomerase II-DNA cleavable complex. Through both experiments. DNA relaxation assay by the increment of topoisomerase II concentration and DNA unwinding assay, it was shown that SJ5b and SQ7b did not interact with topoisomerase II itself but bound to DNA. Therefore, it was concluded that DNA binding of SJ5b and SQ7b caused the inhibition of topoisomerase II related to DNA relaxation but no or very weak stabilization of topoisomerase II-DNA cleavable complex. In addition, SJ5b and SQ7b prevented whole cell nucleic acid syntheses in HL60 cells.

• 대한화학회지
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• 제54권6호
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• pp.723-726
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• 2010

마이크로 반응을 이용하여 $NaHSO_4/SiO_2$을 촉매로 하는 solvent-free 합성을 통하여 $\beta$-enaminone 과 2-methylquinolin-4(1H)-one 및 그 유도체를 합성하는 효율적인 방법을 개발하였다. 반응 시간이 짧고, 수율이 좋았으며, 마이크로웨이브를 사용하지 않는 반응보다는 높은 선택성, 간단성, 무용매 반응 및 친환경적인 반응이다.

• 약학회지
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• 제40권2호
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• pp.131-134
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• 1996

3,4-Dimethoxyphenethyl amine(1) and 3,4-dimethoxybenzaldehyde were converted to compounds(4) through sucessive condensation and reduction reaction. Compound(4) was treated with methylthioacetyl chloride to give compound(5) then m-chloroperbenzoic acid(m-CPBA) treatment of compound(5) produced S-oxide(6). To obtain isoquinoline derivative(7),(8), compound(6) were treated with p-TsOH. Xylopinine(9) and it's derivatives(10) were produced by Bischler-Napieralski reaction.

• 대한화학회지
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• 제9권1호
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• pp.37-40
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• 1965

8-Hydroxyquinoline-5-sulfonic acid 를 alkali 媒質에서 $10^{\circ}C$以下로 維持하여 nitroso 化시켜 7-nitroso-8-hydroxy-quinoline-5-sulfonate (NHQS)를 合成하였으며 그 酸解離定數를 分光光度法과 pH滴定法에 依하여 測定하였다. 두 方法에 依하여 近似하게 같은 값은 얻어졌고 이것들은 8-hydorxyquinoline의 該當 pK값에 比해 작다. 8-hydroxyquinoline에 比해 NHQS의 낮은 鹽基性은 導入된 電子吸引性基들의 影響으로 생각되며 特히 nitroso 基는 ortho位의 phenol性 OH基의 酸性度의 增加에 많은 影響을 주는 것으로 생각된다.

• 약학회지
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• 제41권5호
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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.

• 약학회지
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• 제40권1호
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• pp.19-24
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• 1996

The 6,7-dichloroquinolone-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-quin oline-5,8-dione(II). When this compound II was reacted with some alkylamine (methylamine, ethylamine, propylamine, isopropylamine, cyclopropylamine, methoxyethylamine, ethanolamine, benzylamine, furfurylamine), 1N-alkyl-2-methyl-3-ethoxycarbonyl-pyridino(2,3f)-indole-4,9-dione(IIIa-i) were obtained via intramolecular cyclization.

• Archives of Pharmacal Research
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• 제23권5호
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• pp.450-454
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• 2000

Eight 2-alkylaminosubstituted 5,8-dimethoxy-4-methylquinolines and nine 2-alkylaminosub-stituted or 2,6-disubstituted 4-methylquinoline-5,8-diones were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, HCT15 and SF295).

• Bulletin of the Korean Chemical Society
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• 제32권3호
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• pp.1007-1010
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• 2011

$Ir(dpq/dpqx)_2$(przl-R) complexes were prepared and their electrochemical properties were investigated, where dpq, dpqx and przl-R represent 2,3-diphenylquinoline, 2,3-diphenylquinoxaline and N-phenyl-R-pyrazolonate derivatives, respectively. The iridium complexes containing dpq and dpqx as main ligands were reported to show red phosphorescence, and involvement of a pyrazolonate ancillary ligand in the iridium complexes led to high luminous efficiency for organic light-emitting diodes. In this study, we synthesized red phosphorescent iridium complexes containing a new pyrazolonate ancillary ligand and investigated the HOMOs, LUMOs and resulting electrochemical gaps of $Ir(dpq/dpqx)_2$(przl-R) by cyclic voltammetry. The emission wavelengths of the complexes at 600 - 640 nm were consistent with the gaps of 1.95 - 2.03 eV measured from reduction and oxidation potentials of the complexes.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of International Convention of the Pharmaceutical Society of Korea
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• pp.132.1-132.1
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• 2001

• 농약과학회지
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• 제7권4호
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• pp.302-309
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• 2003

신규 화합물 triazolyl quinoline 유도체 230여개의 벼 도열병, 벼 잎집무늬마름병, 토마토 잿빛곰팡이병, 토마토 역병, 밀 붉은녹병과 보리 흰가루병에 대하여 방제효과를 조사하고, 녹병과 흰가루병에 대하여 예방효과가 우수한 KSI-4315와 KSI-4317을 선발하여 밀 붉은녹병과 보리 흰가루병에 대한 작용 특성을 실험하였다. Triazolyl quinoline 유도체인 KSI-4315와 KSI-4317 두 화합물은 구조에서 탄소 4번 위치에 각각 MeS moiety와 MsO moiety를 가진 화합물이다. 두 화합물은 밀 붉은녹병과 보리 흰가루병에 대하여 우수한 예방효과와 치료효과를 나타냈다. KSI-4317은 보리 흰가루병에 대하여, KSI-4315 는 밀 붉은녹병에 대하여 더 높은 예방효과와 치료효과를 보였다. 또한 두 화합물은 지속성도 우수하였다. 밀 붉은녹병에 대하여는 두 약제가 유사하였으나, KSI-4317은 보리 흰가루병에 대하여 특히 약효 지속성이 뛰어나 약제처리 7일 후 에 접종하여도 90% 이상의 방제가를 보였다. 약제의 침투이행성을 엽육이행, 엽간이행과 뿌리로부터 지상 부로의 침투이행에 대하여 실험한 결과, 밀에서 KSI-4315와 KSI-4317은 거의 침투 이행하지 않았으나, 보리에서는 KSI-4315 보다 KSI-4317이 높은 침투이행성을 보였다. 이상의 결과로부터 KSI-4317은 포장에서 밀 붉은녹병과 보리 흰가루병을 효과적으로 방제하리라 생각된다.