• 제목/요약/키워드: 2a

검색결과 421,514건 처리시간 0.199초

Synthesis and Antitumor Evaluation of cis-(1,2-Diaminoethane) dichloroplatinum (II) Complexes Linked to 5- and 6-Methyleneuracil and -uridine Analogues

  • Kim, Jack-C.;Lee, Min-Hwa;Choi, Soon-Kyu
    • Archives of Pharmacal Research
    • /
    • 제21권4호
    • /
    • pp.465-469
    • /
    • 1998
  • The search for platinum (II)-based compounds with improved therapeutic properties was prompted to design and synthesize a new family of water-soluble, third generation cis-diaminedichloroplatinum (II) complexes linked to uracil and uridine. Six heretofore unreported uracil and uridine-platinum (II) complexes are; [N-(uracil-5-yl-methyl)ethane-1,2-di-amine]dichloroplatinum (II) (3a), [N-(uracil-6-yl-methyl)ethane-1,2-diaminel dichloroplatinum (II) (3b), t[N-($2^1$, $3^1$,$5^1$-tri-O-acetyl)uridine-5-yl-methyl] ethane-1,2-diamineldichloroplatinum (II) (6a), {[N-($2^1$,$3^1$, $5^1$-tri-O-acetyl) uridine-6-yl-methyl]ethane-1,2-diamine)dichloroplatinum (II) (6b),[N-(uridine- 5-yl-methyl)ethane-1,2-diamine]dichloroplatinum (II) (7a), [N-(uridine-6-yl- methyl)ethane-1,2-diamine]dichloroplatinum (II) (7b). These analogues were prepared from the key starting materials, 5-chloromethyluracil (1a) and 6-chloromethyluracil (1b) which were reacted with ethylenediamine to afford the respective 5-[(2-aminoethyl)aminol methyluracil (2a) and 6-[(2-aminoethyl)amino]methyluracil (2b). The cis-platin complexes 3a and 3b were obtained through the reaction of the respective 2a and 2b with potassium tetrachloroplatinate (II). The heterocyclic nucleic acid bases 1a and 1b were efficiently introduced on the .betha.-D-ribose ring via a Vorbruggen-type nucleoside coupling procedure with hexamethyldisilazane, trimethylchlorosilane and stannic chloride under anhydrous acetonitrile to yield the stereospecific .betha.-anomeric 5-chloromethyl- $2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4a) and 6-chloromethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4b), respectively. The nucleosides 4a and 4b were coupled with ethylenediamine to provide the respective 5-[(amino-ethyl)aminolmethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5a) and 6-[(aminoethyl)amino] methyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5b). The diamino-uridines 5a and 5b were reacted with potassium tetrachloroplatinate (II) to give the novel nucleoside complexes, 6a and 6b, respectively which were deacetylated into the free nucleosides, 7a and 7b by the treatment with CH$_{3}$ONa. The cytotoxic activities were evaluated against three cell lines (FM-3A, P-388 and J-82) and none of the synthesized compounds showed any significant activity.

  • PDF

IDEALS IN A TRIDIAGONAL ALGEBRA ALGL

  • LEE, SANG KI;KANG, JOO HO
    • Journal of applied mathematics & informatics
    • /
    • 제34권3_4호
    • /
    • pp.257-267
    • /
    • 2016
  • We find examples of Ideals in a tridiagonal algebra ALGL and study some properties of Ideals in ALGL. We prove the following theorems: Let k and j be fixed natural numbers. Let A be a subalgebra of ALGL and let A2,{k} ⊂ A ⊂ {T ∈ ALGL | T(2k-1,2k) = 0}. Then A is an ideal of ALGL if and only if A = A2,{k} where A2,{k} = {T ∈ ALGL | T(2k-1,2k) = 0, T(2k-1,2k-1) = T(2k,2k) = 0}. Let B be a subalgebra of ALGL such that B2,{j} ⊂ B ⊂ {T ∈ ALGL | T(2j+1,2j) = 0}. Then B is an ideal of ALGL if and only if B = B2,{j}, where B2,{j} = {T ∈ ALGL | T(2j+1,2j) = 0, T(2j,2j) = T(2j+1,2j+1) = 0}.

Photopic과 Scotopic 곡선의 분포함수 유도 및 분석 (A Distribution Function Analysis of Photopic and Scotopic Curves)

  • 김용근
    • 한국안광학회지
    • /
    • 제5권2호
    • /
    • pp.157-161
    • /
    • 2000
  • 광원의 세기가 다른 조건하에서 눈의 시감효율은 추상체와 간상체에 의해 파장에 따라 2개의 함수로 이루어진다. 광자에 대한 추상체-간상체의 반응확률을 이용하여 $P({\lambda})=A{\cdot}e^{-({\lambda}-{\lambda}_0)^2/2W^2}$의 분포함수 수식을 유도하였다. 이 식은 파장에 따른 CIE의 눈의 시감효율 곡선에 잘 적용되며 상대 시감효율의 경우 photopic의 경우 A=106.4, ${\lambda}_0=559.2$, W=83.5이고 scotopic의 경우 A=99.3, ${\lambda}_0=502.6$, W=79.5의 값을 얻었다. 1m/W의 단위를 사용하는 시감효능 곡선에서는 photopic의 경우 $A=7.2{\times}10^4$, ${\lambda}_0=559.2$, W=86.5이고 scotopic의 경우 $A=1.6{\times}10^5$, ${\lambda}_0=502.6$, W=79.5의 값을 얻었다.

  • PDF

ISOMORPHISM CLASSES OF HYPERELLIPTIC CURVES OF GENUS 2 OVER $F_{2_}{N}$ FOR EVEN n

  • Park, Chun-Soo;Rhee, Min-Surp
    • Journal of applied mathematics & informatics
    • /
    • 제13권1_2호
    • /
    • pp.413-424
    • /
    • 2003
  • L. H Encinas, A. J. Menezes and J. M. Masque in [3] proposed a classification of isomorphism classes of hyperelliptic curve of genus 2 over finite fields with characteristic different from 2 and 5. Y. Choie and D. Yun in [2] obtained the number of isomorphic classes of hyperelliptic curves of genus 2 over $F_{2-}$ using direct counting method. We have obtained isomorphism classes of hyperelliptic curves of genus 2 over $F_{2n}$ for odd n, represented by an equation of the form $y^2$ + $a_{5}$ y = $x^{5}$ + $a_{8}$ x + $a_{10}$ ( $a_{5}$ $\neq$0) [1]. In this paper we characterize hyperelliptic curves of genus 2 over $F_{2n}$ for even n, represented by an equation of the form $y^2$ + $a_{5}$ y = $x^{5}$ + $a_{5}$ x + $a_{10}$ ( $a_{5}$ $\neq$0).>0).

Tris(tetraethylammnnium) [bis(trimetaphosphate $\kappa^3O, O^', O^{"}$)] Vamdate(3-),$[V(P_3O_9)_2](NC_8H_{20})_3$,의 두가지 가능한 공간군 (Two Possible Space Groups of Ttis(tekaethylammonium) [bis(trimetaphosphate $\kappa^3O, O^', O^{"}$)] Vanadate(3-),$[V(P_3O_9)_2](NC_8H_{20})3$)

  • 서일환;이진호
    • 한국결정학회지
    • /
    • 제5권1호
    • /
    • pp.1-6
    • /
    • 1994
  • 화합물 VP6N3018C243H60의 두 가지 가능한 공간군은 PT,a=14.O22(1), b=12.644(2), c=12.640(1)A, a=80.38(1), β=102.12(1), y =102.16(1), V=2124.1A3, Z=2, u=0.47cm-1,d==1.46g/cm3, Fo>4c IfoI인 3350윤의 독립반사강도에 대하여 R=0.083 과 C2/c, a=19.32(2), b=16.32(2), c=14.02(1)A, β= 105.98(5), V=4348.2A3, Z=4, Fo>4o IFoI인 1590개의 독립반사강도에 대하여 R=0.083 이다. 주간군 Pi의 경우 단위포내에 두 분자가 있는데 각 분자내의 바나둠 원자가 특수치치에 있어 중심대칭에 의하여 한 분자를 이루고 있으므로 단위포내의 비대칭단위는 두개의 bis(timetalhosphate)vanadate 반분자와 3개의 tetraethylammDnium분자로 되어있다. 공문군 C2/c의 경우 bis(trimetaphosphate)vanadate 한분자의 vanadium 원자가 중심대1칭을 갖는 변광단동치에 있으며, 3개의 tetrethylammonium 분자중 한 분자내의 CL2, N2, C25 원자들을 2-회회전대칭축이 지나므로 bis(trimetaphosphate)vanadate 반분자와 tetraethylammonium 3/2 분자가 비대칭단위를 이루고 있다. 두 경우 공히 vanadium원자를 배위하고 있는 6개의 산소원자가 8함체를 이루며 nitrogen원자와 결합하고 있는 4개의 carbon 원자들은 모두 disorder되어 있어 nitrogen원자의 주권에 있는 8개의 carbon 원자들은 불규칙한 12면체를 이루고 있다.

  • PDF

Fusarium graminearum의 ZEB2 동형단백질에 의한 지랄레논 생합성 자가조절

  • Park, Ae Ran;Lee, Yin-Won
    • 한국균학회소식:학술대회논문집
    • /
    • 한국균학회 2016년도 춘계학술대회 및 임시총회
    • /
    • pp.27-27
    • /
    • 2016
  • The ascomycete fungus Fusarium graminearum is the most common pathogen of Fusarium head blight (FHB), a devastating disease for major cereal crops worldwide. FHB causes significant crop losses by reducing grain yield and quality as well as contaminating cereals with trichothecenes and zearalenone (ZEA) that pose a serious threat to animal health and food safety. ZEA is a causative agent of hyperestrogenic syndrome in mammals and can result in reproductive disorders in farm animals. In F. graminearum, the ZEA biosynthetic cluster is composed of four genes, PKS4, PKS13, ZEB1, and ZEB2, which encode a reducing polyketide synthase, a nonreducing polyketide synthase, an isoamyl alcohol oxidase, and a transcription factor, respectively. Although it is known that ZEB2 primarily acts as a regulator of ZEA biosynthetic cluster genes, the mechanism underlying this regulation remains undetermined. In this study, two isoforms (ZEB2L and ZEB2S) from the ZEB2 gene in F. graminearum were characterized. It was revealed that ZEB2L contains a basic leucine zipper (bZIP) DNA-binding domain at the N-terminus, whereas ZEB2S is an N-terminally truncated form of ZEB2L that lacks the bZIP domain. Interestingly, ZEA triggered the induction of both ZEB2L and ZEB2S transcription. In ZEA producing condition, the expression of ZEB2S transcripts via alternative promoter usage was directly or indirectly initiated by ZEA. Physical interaction between ZEB2L and ZEB2L as well as between ZEB2L and ZEB2S was observed in the nucleus. The ZEB2S-ZEB2S interaction was detected in both the cytosol and the nucleus. ZEB2L-ZEB2L oligomers activated ZEA biosynthetic cluster genes, including ZEB2L. ZEB2S inhibited ZEB2L transcription by forming ZEB2L-ZEB2S heterodimers, which reduced the DNA-binding activity of ZEB2L. This study provides insight into the autoregulation of ZEB2 expression by alternative promoter usage and a feedback loop during ZEA production.

  • PDF

(펜타메틸시클로펜타디에닐) 비스(포스핀)루테늄의 염화물과 수소화물 유도체 (Chloro- and Hydrido Complexes of (Pentamethylcyclopentadienyl) bis(phosphine)ruthenium)

  • 이동환
    • 대한화학회지
    • /
    • 제36권2호
    • /
    • pp.248-254
    • /
    • 1992
  • 에탄올 용매 중에서, 착물 $[({\eta}^5-C_5Me_5)RuCl_2]_2$ (1)에 대하여 과량의 포스핀을 반응시켜 비스(포스핀)루테늄 유도체$({\eta}^5-C_5Me_5)Ru(PR_3)_2Cl(PR_3=PMe_3,\; PMe_2Ph,\;PEt_3,\;PMePh_2$, 1/2DPPE, 1/2DPPB) (2a${\sim}$2f)를 합성하였다. 이 유도체들은 에탄올 용매 중에서 $NaBH_4$와 반응하여 상응하는 황색의 착수소화물 $({\eta}^5-C_5Me_5)Ru(PR_3)_2Hl(PR_3=PMe_3,\;PEt_3,\;PMePh_2$, 1/2 DPPE, 1/2DPPB) (3a${\sim}$3e)을 생성한다. 착염화물 (2a${\sim}$2f)와 착수소화물 (3a∼3e)는 모두 결정으로 얻어졌으며, IR, $^1H-NMR$ 그리고 원소분석으로 동정되었다.

  • PDF

칼슘 이온으로 완전히 치환된 제올라이트 A의 탈수 구조와 칼슘 치환 제올라이트 A에 요오드가 흡착된 착물 구조 (The Structures of Dehydrated Fully $Ca^{2+}$-Exchanged Zeolite A and of Its iodine Sorption Complex)

  • 장세복;한영욱;김덕수;김양
    • 한국결정학회지
    • /
    • 제1권2호
    • /
    • pp.76-83
    • /
    • 1990
  • 완전히 Ca2+ 이온으로 치환된 탈수구조(a=12 2f3(2) .41와 이 결정에 요오드가 흡착된 구조(a= 12.258(2) 입)를 21살에서 입방공간군 Pm3m를 사 용하여 단결정 X-선 회절법으로 구조를 해석하였다. 탈수구조는 I>3 w (I)인 206개의 반사를 사용하 여 Rw값이 0.081까지 정밀화되었고 요오드가 흡착 된 구조는 173개의 반사를 사용하여 Rw값이 0.084 까지 정밀화되었다. 각각의 구조에서 단위세포당 6 개의 Ca2+ 이온은 6-링의 산소와 결합하면서 3개 의 다른 3회 회전축상에 위치하였다. 탈수한 칼슘 치환 제올라이트 A는 80살에서 단위세포당 여섯개의 요오드 분자를 흡착하며 각 요오드 분자는 골조 산소 원자와 전하이동 착물을 형성하였다(I-0=3. 32(3) A, I-I=2.7l (2) A 그리고 I-I-0=180℃).

  • PDF

한국인 대상의 PPARGC1A 유전적 다형성과 제2형 당뇨병과의 상관성 (Association between PPARGC1A Genetic Polymorphisms and Type 2 Diabetes Mellitus in the Korean Population)

  • 진현석;박상욱
    • 대한임상검사과학회지
    • /
    • 제53권1호
    • /
    • pp.81-87
    • /
    • 2021
  • 제2형 당뇨병(T2DM)과 그 유병률은 전세계적으로 증가하고 있다. T2DM은 인슐린 저항성이 높아지고 인슐린 분비가 감소해 발생하는 당뇨병의 가장 흔한 유형 중 하나다. 과산화물 증식활성수용체 감마 공활성제 1 알파(PPARGC1A)는 미토콘드리아 생물 발생의 마스터 조절기와 간에서 포도당신합성에 관여한다. 본 연구에서는 T2DM이 있는 한국인 중년층의 PPARGC1A 유전자의 유전적 다형성을 분석하였다. 그 결과, PPARGC1A 유전자 중 15개의 SNP가 T2DM과 통계적으로 유의한 연관성을 보였으며, 그 중 PPARGC1A 유전자의 rs10212638은 T2DM (P=0.015, OR=1.29, CI=1.05~1.59)과 통계적으로 가장 큰 유의한 상관관계를 보였다. PPARGC1A의 마이너 유전자형(minor allele) G는 T2DM의 위험을 증가시켰다. 본 연구는 T2DM와 PPARGC1A의 유전적 다형성 사이에 유의한 연관성을 보여주고 있다. 이러한 결과는PPARGC1A의 SNP가 T2DM의 병의 원인이 되는 유전적 연관성이 있음을 시사한다.

Disialoganglioside GD2의 Anti-idiotypic Antibody (Ab2)에 의해 유도된 Anti-anti-idiotypic Antibodies (Ab3)의 특성 (Characterization of Anti-anti-idiotypic Antibodies (Ab3) Induced by Immunization of Anti-idiotypic Antibodies (Ab2) Mimicking Disialoganglioside GD2)

  • 박윤선
    • IMMUNE NETWORK
    • /
    • 제3권2호
    • /
    • pp.118-125
    • /
    • 2003
  • Background: Disialoganglioside GD2 is a tumor-associated antigen that is overexpressed on tumor cells of neuroectodermal origin, such as melanoma and neuroblastoma. Anti-idiotypic antibodies that mimic GD2 may induce more effective immune responses than GD2 antigen itself, because they are protein antigens and are known to be able to break immune tolerance. In this study, to explore the potential of anti-idiotypic antibodies as tumor vaccines, the ability of anti-idiotypic antibodies (Ab2) to induce anti-anti-idiotypic antibodies (Ab3) that bind to the original antigen GD2 was investigated. Methods: Six monoclonal anti-idiotypic antibodies (1A8, 1G5, 2B6, 3A4, 3D6, 3H9) to monoclonal antibody M2058, which is a monoclonal antibody to GD2, were produced in mice. Three (1A8, 3A4, 3H9) of them were selected based on their ability to inhibit the binding of Ab1 to D142.34 (murine melanoma cell expressing GD2). These 3 different Ab2 were injected into rabbits, and rabbit Ab3 induced by each of them were characterized. Results: Ab3-containing sera from two rabbits immunized with 1A8, 3A4, or 3H9 bound significantly (P<0.05) to D142.34 but not to B78.96 (GD2-negative cell), and bound significantly (P<0.05) to isolated GD2 but not to GD1a. Ab3-containing sera from two rabbits immunized with 3A4 or 3H9 inhibited significantly (P<0.05) the binding of Ab1 M2058 to D142.34, and inhibited significantly (P<0.05) the binding of Ab1 M2058 to the Ab2. Conclusion: These results suggest that anti-idiotypic antibodies 3A4 and 3H9 have a potential to be used as vaccines against tumors expressing GD2 by inducing GD2-specific antibodies (Ab3).