• Title/Summary/Keyword: L-1210

Search Result 268, Processing Time 0.033 seconds

항암 및 항바이러스성 뉴크레오사이드의 합성

  • 이희주
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1994.04a
    • /
    • pp.228-228
    • /
    • 1994
  • Nucleoside계통의 유도체를 합성하여 체내 DNA 또는 RNA 합성대사에 영향을 줌으로써 궁극적으로 항암성 또는 항 virus성 작용을 나타내는 화합물을 얻고자 하였다. 본 연구에서는 천연의 nucleoside 구조중에서 특히 당부분에 변형을 준 일련의 acyclonucleoside 유도체들을 합성하였다. 이는 그간 많이 연구되어온acyclonucleoside 계열인 acyclovir계와는 달리 ribose 당부분을 $C_1$에서 $C_{5}$까지 거리가 유사한 acycloalkyl 결합형태로 결합하고 3'위치에 변형을 가져온 pyrimidine계 유도체를 합성하고자 일련의 반응을 시도하였다. 목적하는 화합물 계열을 얻지 못하고, 몇종류의 관련 유도체들을 분리하여 구조를 규명하고자 하였고, 이들중 일부에 대해 in vitro L1210 cell 증식억제효과를 검색하여 그 결과를 보고하고자 한다.

  • PDF

항암제의 세포독성에 대한 obakunone의 상승효과

  • 정현주;석대은;배기환;이준성
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1996.04a
    • /
    • pp.164-164
    • /
    • 1996
  • 생약(5kg)을 분말로 한 뒤, MeOH 4$\ell$로 24시간, 2회, 환류추출, 추출액을 감압 농축하여 MeOH ex. (450g)을 얻었다. 이것을 물에 현탁시켜 헥산, 벤젠, 에틸아세테이트, 수층으로 분획, L1210 세포에 대하여 이들 분획물과 vincristine의 병용효과를 관찰하였다. 그 결과, 벤젠분획물에서 강한 효과가 있었으므로 컬럼크로마토그라피하여 물질을 분리하였다.

  • PDF

Synthesis and Biological Effects of Some 5-Heterocyclicmethyl-2'-deoxyurdines

  • Kwak, In-Young;Ryu, Eung K.
    • Archives of Pharmacal Research
    • /
    • v.13 no.4
    • /
    • pp.306-309
    • /
    • 1990
  • The synthesis of 5-hyterocyclimethyl-2'-deoxyuridines (4a-f) has been accomplished by displacement reaction of 5-(bromomethyl)-3', 5'-di-O-acetyl-2'-deoxyuridine with heterocyclic compounds, followed by removal of acetyl protecting group with methanolic ammonia. The compoudns synthesized were evaluated the inhibitory effects on L1210 cell probiferation and antiviral activities against Herpes simplex virus type 1 (HSV-1) None of the compounds exhibited sufficient biological activities.

  • PDF

2-(1-Aminoacetyloxyalkyl)-1,4-Dihydroxy-9,10-Anthraquinone Derivatives: Synthesis and Cytotoxic Activity (2-(1-아미노아세칠옥시알킬)-1,4-디하이드록시-9,10-안트라퀴논 유도체의 합성 및 세포독성 평가)

  • 신동진;유영제;안병준
    • YAKHAK HOEJI
    • /
    • v.45 no.2
    • /
    • pp.133-139
    • /
    • 2001
  • To improve water solubility of 1,4-dihydroxy-9,10-anthraquinone moiety, 23 of 2-(1-aminoacetylalkyl)-1,4-dihydroxy-9,10-anthraquinone derivatives, which contain nitrogen atom, were synthesized. Of the synthesized compounds, 18 compounds were more cytotoxic on L1210 cells than 2-(1-acetyloxyalkyl)-1,4-dihydroxy-9,10-anthraquinone as comparative structure. This result might be due to the increased hydrophilicity of the compounds.

  • PDF

Synthesis and Antitumor Activity of Novel Gericudranin E Derivatives (새로운 항암성 제리쿠드라닌 E 유도체의 합성 및 항암활성)

  • 박재호;박경란;호현순;김희두;표명윤
    • YAKHAK HOEJI
    • /
    • v.43 no.5
    • /
    • pp.559-565
    • /
    • 1999
  • The two gericudranin E derivatives, GER-I & II, were synthesized and evaluated their antitumour activities for the elucidation of structure-activity relationship. 2,4,6-Trihydroxyacetophenone was converted to target molecules GER-I and GER-B in 5 steps via sequential protection, aldol condensation, Michael type-cyclization, regioselective C-benzylation. The cellular growth inhibition of compounds GER-I and GER-II were investigated against P388, L1210, K562, HCT-15, SK-HepG-1, MCF-7 as cancer cell lines and mouse splenocytes as a normal cell by MTT assay.

  • PDF

Synthesis of 1-(Heterocyclic Substituted Anilino)-9H-Thioxanthon-9-ones and Their Antitumor Activity

  • Omar, Mahmoud-T.
    • Archives of Pharmacal Research
    • /
    • v.20 no.6
    • /
    • pp.610-619
    • /
    • 1997
  • Some new 9H-thioxanthen-9-one incorporated into heterocyclic systems such as pyridone 8, pyrazoline 9, pyranone 11, iminopyrane 12, furopyrimidine 17, imidazothiazole 19, thiazole 21, triazine 24 and other related compounds through a para imminophenyl grouping at position-1 of the thioxanthenone ring were synthesized and tested as antitumor agents against L1210 leukemia in mice. Some of the new compounds showed considerable antitumor activity.

  • PDF

Flow Characteristics in Unsteady Boundary Layer on Stator Blade of Multi-Stage Axial Compressor (다단 축류 압축기 정익 흡입면에서의 비정상 경계층 유동 특성)

  • Shin, You-Hwan;Elder, Robin L;Kim, Kwang-Ho
    • Transactions of the Korean Society of Mechanical Engineers B
    • /
    • v.28 no.10
    • /
    • pp.1210-1218
    • /
    • 2004
  • Experimental study was performed to investigate the flow behavior in boundary layer on the blade suction surface of a multi-stage axial flow compressor, which was focused on the third stage of the 4-stage Low Speed Research Compressor. Flow measurements in the boundary layer were obtained using a boundary layer hot wire probe, which was traversed normal to the blade suction surface at small increments by the probe traverse specially designed. Detailed boundary layer flow measurements covering most of the stator suction surface were taken and are described using time mean and ensemble averaged velocity profiles. Amplitude of the velocity fluctuation and turbulence intensity in the boundary layer flow are also discussed. At midspan, narrow but strong wake zone due to passing wake disturbances is generated in the boundary layer near the blade leading edge for the rotor blade passing period. Corner separation is observed at the tip region near the trailing edge, which causes to increase steeply the boundary layer thickness.

Synthesis of 1-(4-Thio-${\alpha},{\beta}$-D-ribofuranosyl)-5-halogenouracils (II). 5-Fluoro-4'-thiouridine and 5-Chloro-4'-thio-uridine (5-할로겐 치환된 Uracil의 4-Thiosugar Nucleosides의 합성에 관한 연구 (제2보). 5-Fluoro-4'-thiouridine과 5-Chloro-4'-thiouridine의 합성)

  • Jack C Kim;Won-Jei Cho;Miroslay Bobek;Roy L. Whistler
    • Journal of the Korean Chemical Society
    • /
    • v.19 no.6
    • /
    • pp.438-442
    • /
    • 1975
  • The syntheses of anomeric mixtures of 1-(4-thio-${\alpha},{\beta}$-D-ribofuranosyl)-5-fluoro-and 5-chlorouracils from their corresponding bis(trimethylsilyl) derivatives of 5-halogenouracils and 2,3,5-tri-O-acetyl-4-thio-${\alpha},{\beta}$-D-ribofuranosyl chloride are described. Preliminary biochemical studies showed that in leukemia 1210 cells and Streptococcus faecium, the ${\beta}$-anomeric 5-chloro-4'-thionucleoside is not greatly different from the corresponding 4'-oxygen analog. However, the 5-fluoro-4'-thionucleoside showed a growth inhibitory effect more than that of the oxygen counterpart. The potential chemotherapeutic use of the analog is to warrant further study.

  • PDF

Cytotoxic Saponins from the Root of Dipsacus asper Wall

  • Hung Tran Manh;Jin WenYi;Thuong Phuong Thien;Song Kyung Sik;Seong Yeon Hee;Bae KiHwan
    • Archives of Pharmacal Research
    • /
    • v.28 no.9
    • /
    • pp.1053-1056
    • /
    • 2005
  • Cytotoxic activitiy of seven hederagenin saponins isolated from the root of Dipsacus asper were investigated in vitro against L1210, HL-60 and SK-OV-3 tumor cell lines by the MTT method. $3-O-\alpha-L-rhamnopyranosyl-(1{\rightarrow}2)-\alpha-L -arabinopyranosyl$ hederagenin (2),\;$3-O-\beta-D­xylopyranosyl-( 1{\rightarrow}3)-\alpha-L-Rhamnopyranosyl-(1{\rightarrow}2)-\alpha-L -arabinopyranosyl$ hederagenin (6) and $3-O-\beta-D-glucopyranosyl-(1{\rightarrow}3)-\alpha-L-rhamnopyranosyl-( 1{\rightarrow}2)-\alpha-L-arabinopyranosyl$ hederagenin (7) exhibited the potent cytotoxicity against the three tumor cell lines with $IC_{50}$ values ranging from 4.7 to 8.7 ${\mu}g/mL$, with the exception of compound 7, which exhibited weak cytotoxic activity against SK-OV-3 $(IC_{50}\;22.5\;{\mu}g/mL)$. Other compounds did not exhibit any cytotoxic activity $(IC_{50}>30{\mu}g/mL)$.

Antitumor constituents from some Korean medicinal plants

  • Bae, Ki-Hwan
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1998.11a
    • /
    • pp.56-61
    • /
    • 1998
  • For the screening of bioactive natural products, the benzene or methanol extracts from 93 medicinal plants of Korea were prepared, and tested for the cytotoxicity against L1210 cells and for the antitumor action (Bae et al., 1992 and 1996). Of 93 extracts tested, 6 samples showed a cytotoxicity in both benzene and methanol extract, 39 samples in benzene and 13 samples in methanol extract. The benzene extract of the root of Scutellaria indica L., Sophora fIavescens Solander ex Aiton, Carpesium abrotanoides L., Gymnaster koraiensis (Nakai) Kitamura, Pyrola japonica Klenze, and Forsythiae Fructus showed a potent cytotoxic activity. This observation led to isolate active cytotoxic components, some of which demonstrated some antitumor action. In addition, the structure-activity relationship was discussed.

  • PDF