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약물-고분자물질 결합체 합성연구 : 5-Fluorouracil과 사람의 혈청 Albumin 및 Poly-L-lysine 결합체 합성
이희주,신혜순,이명걸,박만기,김종국,Lee, Hee-Joo,Shin, Hae-Soon,Lee, Myung-Gull,Park, Man-Ki,Kim, Chong-Kook 대한약학회 1989 약학회지 Vol.33 No.5
The durg-macromolecule conjugates i.e. 5-fluorouracil-1-acetyl-human serum albumin(FU-AA-HSA, 8) and 5-fluorouracil-1-acetyl-poly-L-lysine(FU-AA-polylys, 9) have been synthesized and purified by sephadex G-25 gel filtration with 0.05M phosphate buffer(pH 7.5). The analyses of conjugates gave the molar ratio of FU-AA : HSA of 70-100:1 and FU-AA: poly-L-lysine of 109:1. The weight percent of FU-AA(as $FU-CH_2CO-$) in FU-AA-HSA conjugate was 16-22% and the one in FU-AA-polylys was 22.4%.
이희주(Hee Joo Lee),신혜순(Hae Soon Shin),진현숙(Hyun Suk Jin),김지현(Ji Hyun Kim),김종국(Chong Kook Kim) 대한약학회 1993 약학회지 Vol.37 No.1
In order to find out a proper connecting bridge between 5-fluorouracil(5-FU) and a macromolecule such as a polypeptide, potentially hydrolytic N1-derivatives of 5-FU have been synthesized and evaluated for their biological activity. When tested with in vitro leukemic L1210 cells all the obtained derivatives exhibited slightly higher antitumor activity than the parent 5-FU. Among them the N1-carbamoyl analogue 2 and N1-acetamido analogue 6b showed 50% inhibition of the L1210 Cell growth at the concentrations of 5.01 X 10-8M and 1.03 X 10-7M, respectively. When tested against sarcoma 180 tumor cells inoculated into mice, the compounds 2 and 6b exhibited, respectively, 62% and 54% inhibition of the solid tumor growth at the 5-time doses of 100 mg/kg/day. Both compounds, N1-carbamoyl analogue 2 and N1-acetamido analogue 6b, released the parent 5-FU when incubated in the L1210 cell cultural media for 5 hrs.
5-Fluorouracil-지질 결합체 합성 및 in vitro 항암효과 평가
이희주(Hee Joo Lee),장판섭(Pan Sup Chang),김재완(Jae Wan Kim),정기화(Ki Hwa Jung),신순희(Soon Hee Shin),신혜순(Hae Soon Shin),정순복(Soon Bog Jung) 대한약학회 1990 약학회지 Vol.34 No.6
The FU-fat conjugates(4a-e) as a prodrug have been synthesized by condensing various fatty acids(1a-e) via isocyanates(2a-e) as carbamoyl group at N1-position of 5-fluorouracil and their structures characterized. Preliminary testing for their antitumor effect was carried out on leukemia L1210 cells in culture. Most of them(4a-d) like the parent FU exhibited less than 50% inhibition on grouth of the cultrued cells at the concentration of 1X10-7M. Only a dicarboxylic acid derivative, 4e, showed over 50% inhibition at the same level.
신혜순,박해선,박명숙 德成女子大學校 藥學硏究所 2003 藥學論文誌 Vol.14 No.1
For the selective candidates of COX-2 inhibitors, we designed new NSAIDs which is the hydantoin ring based structure substituted with two planar aromatic ring. Seven O-alkyl a-anilinophenylacetate were synthesized through the base-catalysis hydrolysis of 1,5-diarylhydantoins and O-alkylation of sodium a- anilinophenylacetate with alkyl halides. To evaluate inhibitory effect of COX-2. synthetic hydantoin ring based derivatives were screened with accumulation of prostaglandin by lipopolysaccharide in aspirin-treated murine macropharge cell. Most of these compounds inhibited less than 60% of the prostaglandin E_(2) production at a concentration of 10μg/mL.
Diazaanthrine 유도체의 prostaglandin synthase-2 저해활성
신혜순 德成女子大學校 藥學硏究所 2001 藥學論文誌 Vol.12 No.1
A series of diazaanthrine derivatives (3a-3e) as new analogues of tacrine has been prepared. This series has been tested for their ability to inhibit prostaglandin synthase-1 and 2 isoforms. This series has shown potent in vitro inhibition of the enzyme prostaglandin synthase-2 with % inhibition=70.3∼23.6 at 10 ㎍/㎖. Compound 3b was the most potential inhibitor with an IC_50s=15.6 ㎍/㎖. Derivatives 3a and 3c displayed weak in vitro inhibition of prostaglandin synthase-2 with IC_50s 20.2∼29.2 ㎍/㎖. The most selective compound was 3b with a prostaglandin synthase inhibitory activity of 1/2 in excess of 5 times. These data indicate that 3b is an prostaglandin synthase-2 inhibitor with good selectivity as the drug of Alzheimer's disease.
Cyclooxygenase-2 저해제로서의 benzothiazine 유도체 합성과 항염작용 평가
신혜순,박명숙,권순경 德成女子大學校 藥學硏究所 2000 藥學論文誌 Vol.11 No.1
The antiinflammatory mechanism of NSAIDs is attributed to the reduction of prostaglandin synthesis by the direct inhibition of cyclooxygenase. Inhibition of prostaglandin production in organs such as stomach and kidney can result in gastric lesions, nephrotoxicity and increased bleeding. In this study, newly designed COX-2 inhibitors, synthesized 1,2-benzothiazine derivatives, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. Lead compounds in the structure-activity relationship were studied to synthesize new highly selective COX-2 inhibitors. To determine inhibitory effect of COX-2, synthesized 1,2-benzothiazine derivatives were screened with accumulation of prostaglandin by lipopolysaccharide (LPS) in aspirin-treated macrophages and murine macropharge cell. Some of synthesized 1,2-benzothiazine derivatives were shown to be effective as selective COX-2 inhibitory activity. Others exhibited a preferential inhibition of COX-2, although some COX-1 inhibitory activity was still present. As a conclusion, simple monomer derivatives were more active than dimer derivatives. Substitution of halogen (Br, Cl) on the benzothiazine nucleus slightly enhanced inhibition activity.
신혜순,이희주 德成女子大學校 藥學硏究所 1990 藥學論文誌 Vol.1 No.1
Drug-macromolecule conjugates, i.e., 5-fluorouracil-1-acetyl-poly-L-lysine (FU-AA-poly-L-lys) and methotrexate-poly-L-lysine (MTX-poly-L-lys) have been synthesized. The analyses of conjugates gave the molar ratio of FU-AA: Poly-L-lysine of 109:1 and MTX: poly-L-lysine of 16:1. The weight percent of FU-AA (as FU-CH_2CO)-in FU-AA-poly-L- lysine conjugate was 22.4% and the one of MTX in MTX-poly-L-lysine was 13%.
COX-2 Inhibitors를 위한 새로운 1,2-치환된 피롤리딘 유도체의 합성
박명숙,신혜순 德成女子大學校 藥學硏究所 2000 藥學論文誌 Vol.11 No.1
For the development of new COX-2 inhibitor, novel compounds were synthesized through induction an arylsulfony group to 1-position, an arylcarboxamidyl group to 2-position and an aralkyl group to 4-position of L-proline. The 4-aralkyloxy-1-(4-methylphenylsulfonyl)-L-prolines 5a-d were synthesized through N-tosylation, esterification, O-alkyl-(or aryl)ation, base-hydrolysis (deprotection of carboxylic acid) from 4-hydroxy-L-proline. Final 4-aralkyloxy-1-(4-methylphenylsulfonyl)-2-phenylcarboxamidyl-L-prolines 6a-d were synthesized through the condensation of aniline with 5a-d using DCC.
플라바논의 아자 유도체인 새로운 2,3-디하이드로-2-페닐-4-퀴놀론 유도체의 간편한 합성 : Aza Analogs of Flavanones
박명숙,신혜순 德成女子大學校 藥學硏究所 2003 藥學論文誌 Vol.14 No.1
A series of 2,3-dihydro-2-phynyl-4-quinolones 6a-c have been synthesized using acid-catalyzed one-pot reaction. 2,3-Dihydro-2-phyenylquinolone was synthesized from aniline by condensation with ethyl benzoylacetate followed by a cyclization in toluene. Similarly, the 6-substituted 2,3-dihydro-2-phylquinolones were prepared from the para-substituted aniline. The reaction mechanism of the formation of the final product involves the nucleophilic dehydration and following cyclization between aniline and ethyl benzoylacetate. Nucleophilic dehydration, the condensation was undertaken with p-toluenesulfonic acid at 90-110℃ in toluene for 2-6 hours under the dean-stark apparatus for the ester 3. The ester 3 was continuously converted to the 2-phenylquinolones 6 with dihydrogenation and removal of ethanol. All synthetic process from anilines and ethyl benzoylacetate to 2,3-dihydro-2-phenyl-4-quinolones 6a-c could be carried out in one-pot reaction.
이희주,신혜순,진현숙,김지현,김종국 德成女子大學校 藥學硏究所 1993 藥學論文誌 Vol.4 No.1
In order to find out a proper connecting bridge between 5-fluorouracil(5-FU) and a macromolecule such as a polypeptide, potentially hydrolytic N^1-derivartives of 5-FU have been systhesized and evaluated for their biological activity. When tested with in vitro leukmic L_1210 cells all the obtained derivartives exhibited slightly higher antitumor activity than the parent 5-FU. Among them the N^1-carbamoyl analogue 2 and N^1-acetamido analogue 6b showed 50% inhibition of the L_1210 cell growth at the concentrations of 5.01×10^-8 M and 1.03×10^-7 M, respectively. When tested against sarcoma 180 tumor cells inoculated into mice, the compounds 2 and 6b exhibited, respectively, 62% and 54% inhibition of the solid tumor growth at the 5-time doses of 100 ㎎/㎏/day. Both compounds, N^1-carbamoyl analogue 2 and N^1-acetamido analogue 6b, realeased the parent 5-FU when incubated in the L_1210 cell cultural media for 5 hrs.