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《化学通报》1974,(6)
近些年来,随着核酸化学的发展,已经设计并合成了一系列对恶性肿瘤、病毒以及心血管疾病有较好疗效的核酸类药物。已有报告 N~6-(3-甲基-2-丁烯基)腺苷能抑制艾氏腹水癌和淋巴白血病 L1210的生长。初步临床试验证明,它对患急性骨髓性白血病的儿童产生血象的和临床的缓解作用,而其对肝脏的损害是可逆性的。无产阶级文化大革命以来,工业战线广大职工遵照毛主席关于开展综合利用的指示,广泛地开展了对发酵工业副产物核糖核酸的综合利用的研究工作。在这些工作的推动下,我们也开始把抗肿瘤药物的研究与核酸的综合利用结合起来,把寻找新药的研究和试制已知药物结合起来。我们七四届工农兵学员在毕业 相似文献
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以腺苷为母体,对其N6-位进行结构改造,首先经邻位双羟基保护,N6-位氯代,再在N6-位引入哌嗪环制得中间体2',3'-异丙叉-6-哌嗪嘌呤核苷(4);4与N-氯乙酰苯胺类似物(6a~6h)偶联后脱除邻位双羟基保护合成了8个新型的N6-哌嗪取代腺苷衍生物(8a~8h),其结构经1H NMR,13C NMR和HR-ESI-MS表征。采用MTT法研究了8a~8h对Hela肿瘤细胞的抑制活性。结果表明:大部分目标化合物对Hela肿瘤细胞具有较好的抑制活性,其中2-{4-[9-(3,4-二羟基-5-羟甲基-四氢呋喃-2-基)-9H-嘌呤-6-基]-哌嗪-1-基}-N-(3-氟苯基)-乙酰胺(8e)的活性最好,IC50为21.74μmol·L-1。 相似文献
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SomeLigulariaspecieshavelongbeenusedasfolkremediesduetotheirantibiotic,antiphlogisticandantitumoracti.ities'.Compound1',anovelconiferylalcoho1,wasisolatedfromLigulariaduciformis(Compsitae)alongwiththreenewstructuressuchas2,3,4(Figure1).Thegeometricalstructureof1,deterndnedbyspectroscopictechniques,correspondedto4-o-(6'-hydroxy-7'(9')-dehydro-6coniferylalcohol.ButitsabsoluteconfigurationatC-6'hasnotyetbeendetermined.Hereinwereportthetotalsynthesisof(6'S)-(-)-lfromgeraniol5throughninesteps(Sc… 相似文献
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PseudolaricacidA(l)whichexhibitsantifungalandantifertilityactivitieswasisolatedfromPeudolarl-xKaenlpjbriGord'.Theabsoluteconfigurationsofthesechiralcenterswereassignedtobe3S,4S,10RandIIRrespectively'.Accordingtotheretrosyfltheticanalysis.theskeletonofIcouldbeconstructedbyintramolecular[4- 31cycloadditiontyomaseven-memberedlactone2(Schemel)whichcouldbeobtainedfrom(6S)-6-Thesynthesisbeganwithbetalprotected0-ketoacid4,tbllowedbyamidationwith(-)-camphorsultamandDCCtoobtainapairofdiastereomer… 相似文献
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SynthesisandStructureof4,5-bis(2,4-Dinitrophenylthio)-1,3-Dithiole-2-ThioneQuZheng;CaiJing-Hua;FangQi;YouXiao-Zeng(Coordinati... 相似文献
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The title compound (2E,3E)-N1,N2-bis(2,3,4-trimethoxy-6-methylbenzylidene)- ethane-l,2-diamine (C24H32N2O6, Mr = 444.52) was synthesized and characterized by elemental analysis, IR spectra and single-crystal X-ray diffraction. The crystal belongs to triclinic, space group P2/c, with a = 8.5480(10), b = 9.3710(12), c = 15.280(2)A, β = 90.780(2)°, V= 1223.9(3)A3, Z = 2, Dc= 1.206 g/cm3, 2 = 0.71073A,μ(MoKa) = 0.087 mm^-1, F(000) = 476, the final R = 0.0680 and wR = 0.1450 for 2144 observed reflections with I 〉 2σ(I). X-ray diffraction analysis reveals that the molecule adopts an E configuration about the central C=N functional bond. The phenyl rings of two 2,3,4-trimethoxy-6-methylbenzaldehyde groups are symmetrically parallel. The molecules are linked through C-H…O hydrogen bonding interactions. The title compound possesses moderate antibacterial activity. 相似文献
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研究了3-(2'-苯基-1', 2', 3'-连三唑-4'-基)-4-氨基-5-巯基-1, 2, 4-三唑(1)与取代苯甲酸和脂肪酸(2a-r)在POCl3催化下的反应, 共合成得到18个新的3-(2'-苯基-1', 2', 3'-连三唑-4'-基)-6-烷基/芳基-均三唑并[3, 4-b]-1, 3, 4-噻二唑(3a-r), 经元素分析,IR, 1H NMR和MS进行了结构确证。 相似文献
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Zhi Liang SHANG Zhi Cai SHANG* Qing Sen YU Department of Chemistry Zhejiang University Hangzhou 《中国化学快报》2001,(9)
Crown ether derivatives have been extensively developed to provide enhanced structural recognition of substrate alkyl-ammonium cations. In particular a number of investigations of complexation of chiral alkylammonium salts by chiral crown ethers have been reported. The enantioselectivity has been applied in the chromatographic resolution of amino acid perchlorates. In general the crown ethers used in these studies have been based upon derivatives of 2, 2′-dihydroxy-1, 1′-binaphthyl1 or deriv… 相似文献
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The new title compound (2E,6E)-2,6-bis(2,3-dimethoxybenzylidene)cyclohexanone (C 24 H 26 O 5,M r=394.45) has been synthesized,and its crystal structure was studied.The title compound crystallizes in the orthorhombic system,space group Pca2 1 with a=17.536(2),b=14.8515(16),c=8.0512(9),V=2096.8(4) 3,Z=4,D c=1.250 g/cm 3,λ=0.71073,μ=0.087 mm-1 and F(000)=840.The structure was solved by direct methods and refined to R=0.0533 and wR=0.1248 from 2727 observed reflections (I > 2σ(Ⅰ)).The title molecules are connected through hydrogen bonds to generate a 3-D supramolecule.The preliminary biological tests showed definitely biological activity for the title compound. 相似文献