尿嘧啶

Furthermore, compared with the tautomerizing processes of uracil, the probability of 5-FU to tautomerize to its enol form is much higher. Based on such facts, the reason why 5-FU is an effective anticancer medicament but with some of toxicity is explained to some extent.

通过与尿嘧啶质子转移过程相比较，发现在各种情况下5-氟尿嘧啶异构化为烯醇式的几率均比尿嘧啶的大，在一定程度上解释了为什么5-氟尿嘧啶具有优良抗癌作用的同时具有一定的毒副作用。

In our paper,1-hexylcarbamoyl-5-fluorouracils and1-cyclohexyl-carbamoyl-5-fluorouracils were prepared through 5-fluorouracil reacting with hexyl isocyanate or cyclohexyl isocyanate by using dimethylaminopyridine as the catalyst.

以5-氟尿嘧啶(5-FU)、正己基异氰酸酯和环己基异氰酸酯为原料，在N，N-二甲氨基吡啶的催化下，通过N-脲化反应制成1-己基氨基甲酰基-5-氟尿嘧啶及1-环己基氨基甲酰基-5-氟尿嘧啶。

Cerebral hemorrhage rat models were established via injection of autologous arterial blood in caudate nucleus. Two days after modeling, 5 μL BrdU-labeled human embryonic NSCs suspension was transplanted at four points surrounding hematoma cavity in the rats. After 1 and 2 weeks, rats were sacrificed. Adjacent sections were doubly stained by BrdU/microtubule-associated protein 2 (MAP-2) and BrdU/glial fibrillary acidic protein.

通过注射自体动脉血到尾状核制作大鼠脑出血模型，出血后2 d将标有5'-溴脱氧尿嘧啶的人胚神经干细胞悬液移植到血肿腔周围的4点，1，2周后处死大鼠，相邻脑组织切片行5'-溴脱氧尿嘧啶/微管相关蛋白2和5'-溴脱氧尿嘧啶/胶质纤维酸性蛋白免疫组织化学双染。

METHODS: Cerebral cortex cells of 8-week aborted human fetus were harvested and cultured in vitro to obtain human embryonic NSCs. Cerebral hemorrhage rat models were established via injection of autologous arterial blood in caudate nucleus. Two days after modeling, 5 μL BrdU-labeled human embryonic NSCs suspension was transplanted at four points surrounding hematoma cavity in the rats.

通过注射自体动脉血到尾状核制作大鼠脑出血模型，出血后2 d将标有5'-溴脱氧尿嘧啶的人胚神经干细胞悬液移植到血肿腔周围的4 点，1，2周后处死大鼠，相邻脑组织切片行5'-溴脱氧尿嘧啶／微管相关蛋白2和5'-溴脱氧尿嘧啶／胶质纤维酸性蛋白免疫组织化学双染。

The dissertation includes two parts as follows:In the first part, the synthesis of the uracil derivatives : 5-methoxyuracil and 5-methyluracil was investigated, and the reaction conditions were optimized, thus the overall yields were higher than before.

本论文分为两大部分：第一部分：对尿嘧啶类衍生物5-甲氧基尿嘧啶和5-甲基尿嘧啶的合成进行了研究，并分别进行了工艺优化设计，使这两个化合物的合成总收率均比原来提高。

Glioma is still one of refractory disease in the neurosurgical field; the development of new primary and adjuvant treatment is vital. Recently, the gene therapy of glioma is developed rapidly and there are many methods about the gene therapy that include: suicide gene therapy, immunologic gene therapy, drug resistangce gene therapy, angiostatin gene therapy and so on. The sucide gene therapy is the most potential approach of antitumer, these nonmammalian genes encode enzyme that convert nontoxic prodrugs into highly toxic metablites. Cells transfected with suicide genes are targeted for specific negative selection, witch can be induced by administrtion of the corresponding produg. Among the enzyme/produg combinations, two of the best characterized system are herpes simplex virus thymidine kinase /ganciclovir and Escherichia coli cytosine deaminase /5-flourocytosine (5-FC). The formor can convert the antiviral nucleoside analogs acyclovir , ganciclovir to their nucleoside monophosphate derivatives, the monophosphate forms are subsequently phosphorylated by endogenus cellular kinases to triphosphates, these molecules are potent inhibitors of DNA synthesis.

近年来脑胶质瘤的基因治疗发展迅速，应运而生的方法有自杀基因、免疫基因、多药耐药基因以及抗血管生成基因等，其中自杀基因被认为是最有前景的基因治疗方法，它又称病毒介导的酶／药物前体疗法，是利用转基因技术将哺乳动物细胞中所不含有的自杀基因转入到哺乳动物肿瘤细胞中，该基因表达的产物可将无毒的药物前体转化为毒性药物，从而选择性杀伤该肿瘤细胞，常用的自杀基因有单纯疱疹病毒-胸苷激酶基因和大肠杆菌胞嘧啶脱氨酶基因，前者催化无毒性抗病毒核苷类似物如丙氧鸟苷、无环鸟苷等成为单磷酸核苷衍生物，然后在内源性细胞激酶作用下转化为具有明显毒性的三磷酸核苷，作为DNA合成链的终止剂和DNA合成酶的抑制剂，干扰细胞DNA的合成；后者编码的胞嘧啶脱氨酶可催化5-氟胞嘧啶（5-FC）脱氨成为5-氟尿嘧啶（5-FU），然后代谢为有毒性的5-氟尿嘧啶-5′三磷酸（5-FUTP）和5-氟-2′脱氧尿嘧啶-5′磷酸（5-FdUTP），5-FUTP通过与UTP竞争性结合而抑制mRNA和tRNA的合成，5-FdUTP则作用于胸苷合成酶，导致TMP衰竭而阻止DNA的合成，最终诱导肿瘤细胞凋亡。

The total energy, standard enthalpy, standard entropy and standard free energy were obtained. The calculations show that 5-fluorouracil and 5-chlorouracil existing as the dione forms are the predominant isomers in the gas and aqueous phases. The entropy effect on the Gibbs free energy of 5-fluorouracil and 5-chlorouracil is very small and there is little significance for the tautomeric equilibria.

Onsager反应场溶剂模型用于水相的计算计算结果表明，5-氟尿嘧啶和5-氯尿嘧啶在气相中和水相中主要以双酮形式存在5-氟尿嘧啶和5-氯尿嘧啶的熵效应小，对互变异构平衡没有显著的影响，而焓变对互变异构产生了主要的影响。

METHODS: Collaborative meta-analyses were undertaken of 194 unconfounded randomised trials of adjuvant chemotherapy or hormonal therapy that began by 1995. Many trials involved CMF (cyclophosphamide, methotrexate, fluorouracil), anthracycline-based combinations such as FAC (fluorouracil, doxorubicin, cyclophosphamide) or FEC (fluorouracil, epirubicin, cyclophosphamide), tamoxifen, or ovarian suppression: none involved taxanes, trastuzumab, raloxifene, or modern aromatase inhibitors.

对194个开始于1995年的关于辅助化疗或激素治疗的随机试验进行meta分析，许多试验包含了CMF(环磷酰胺、氨甲喋呤、氟尿嘧啶)，蒽环药物为基础的联合化疗比如FAC(氟尿嘧啶、阿霉素、环磷酰胺)或FEC（氟尿嘧啶、表阿霉素、环磷酰胺）及他莫昔芬或卵巢去势；无一包含紫杉烷类、赫赛汀、雷洛昔芬及芳香化酶抑制剂。

Fluouricil is usually used as anticancer drug, its derivative, 5-fluoro-uracil-1- acetic acid has good biological activity. Its complexes were presented in literatures. However, the coordination modes of it are paradox in literatures. The single crystal structure was resolved to clarify the confusion. The result indicates the carboxylic group coordinates to zinc ion in unidentate, and the heteroatoms of pyrimidine ring are not involved in coordination. Antitumor activity against SMMC-7721 was also examined.

7.5-氟尿嘧啶是临床上广泛使用的抗癌药物，它的衍生物5-氟尿嘧啶-1-乙酸亦具有良好的生物活性，有关它的金属配合物亦有报道，但其结构指认相当混乱，为此研究了它与锌的配合物单晶结构，证明了5-氟尿嘧啶以单齿羧基与锌配位，而嘧啶环氮并未配位，也研究了它对SMMC-7721细胞株的抗肿瘤作用。

The free energy of solvation is well correlated with the dipole moments of 5-fluorouracil and 5-chlorouracil tautomers.

另外， 详细地将5-氟尿嘧啶和5-氯尿嘧啶与尿嘧啶进行了对比，获得三者最稳定异构体间电子结构异同的有用信息。

As she looked at Warrington's manly face, and dark, melancholy eyes, she had settled in her mind that he must have been the victim of an unhappy attachment.

每逢看到沃林顿那刚毅的脸，那乌黑、忧郁的眼睛，她便会相信，他一定作过不幸的爱情的受害者。

Maybe they'll disappear into a pothole.

也许他们将在壶穴里消失