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chemotherapy
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     Chemotherapy was effective.
     化疗有效。
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     Chemotherapy for Gliomas
     脑胶质瘤的化疗
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  chemotherapy
In recent years, significant progress has been made towards the chemotherapy (and ?prophylaxis) of HIV infections.
      
Efavirenz is a trifluoromethylated inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) that shows good results in anti-HIV chemotherapy.
      
The objective of this paper is to explore the value of bone alkaline phosphatase (BALP) for diagnosing osteosarcoma, evaluating the effect of the chemotherapy, judging the prognosis and supervising the relapse and metastasis.
      
Fifteen cases decreased to normal value in ALP after preoperative chemotherapy, and 34 cases decreased in BALP.
      
It has applied value in the diagnosis of osteosarcoma, reflection of the effect of chemotherapy and forecast the prognosis.
      
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Attempts have been made to prepare less toxic antimonials for use in chemotherapy on Schistosomiasis japonicum. It has been established that 2,3-dimercaptopropanol is a powerful antilewisite because it forms a stable ring compound (Ⅱ) with arsenic. It seems reasonable to suppose that analogous cyclic antimony mercaptides (such as Ⅳ and Ⅴ) should be difficult to dissociate and therefore would be less toxic.

2,3-二疏基丙酸与三氯化锑缩合时形成2-氯-4-羧基-4,5-二氢-1,3-二间硫锑杂茂(Ⅵ:R=H),这个产物的氯原子在水解为羟基时,随同失去一分子水而成为内鹽(Ⅶ)。 2,3-二巯基丁二酸能与酒石酸锑钾起复分解作用,生成环状硫醇盐[4,5-二羧基-4,5-二氢-2-羟基-1,3-二间疏锑杂茂(V)]:但当2,3-二巯基丁二酸与三氯化锑作用,并用碳酸氢钠除去氯化氢时,生成与Friedheim所述“TWSb”(X)成分相同的物质。将内消旋2,5-二巯基已-1,6-二酸与酒石酸锑钾处理时得到4,7-二羧基-1,3-二间硫-2-羟锑杂环庚烷单钾盐(Ⅺ)。这些产物曾用於小白鼠的日本血吸虫病实验治疗,其中Ⅶ及Ⅺ的疗效较酒石酸锑钾为好。

A simple and rapid method is described whereby short-term suspension culture of Yoshida ascites sarcoma cells may be used as a screening tool for anti-tumor substances. The tumor cells were cultivated in a medium consisting of horse serum and Hanks' balanced salt solution; sixty thousand to one hundred thousand cells per ml were used as the initial inocula. Cell-counts were carried out at 24 and 48 hours after addition of the drug and the record of the effect of the drugs was graded mainly with reference to...

A simple and rapid method is described whereby short-term suspension culture of Yoshida ascites sarcoma cells may be used as a screening tool for anti-tumor substances. The tumor cells were cultivated in a medium consisting of horse serum and Hanks' balanced salt solution; sixty thousand to one hundred thousand cells per ml were used as the initial inocula. Cell-counts were carried out at 24 and 48 hours after addition of the drug and the record of the effect of the drugs was graded mainly with reference to the per cent inhibition of the tumor cells. In addition, cytomorphological changes were also noted as complementary criteria. The response of this test system was assessed first by exposing it to five known anti-tumor agents, and it was observed that these compounds exhibited a varying antitumor activity against the cultured cells. In decreasing order of effectiveness they were listed as follows: HN_2, nitromin, novoembichinum, myleran and 6-mercaptopurine. Moreover, 117 drug preparations had been screened with this technique. The results indicated that 41.1% of the 24 synthetic compounds and 38.7% of the 93 extracts of natural medicines were found to be active. As regards the comparison of these in vitro results with the in vivo antitumor effects of the same substances in tumor-bearing animals, it was pointed out that there was some, though not perfect, correlation between these two biological test systems. A discussion on the usefulness of this technique as a large scale cancer chemotherapy screening procedure had been made, and its limitations were also presented.

本文介紹利用短期体外培养吉田腹水肉瘤細胞进行药物篩选的方法.所用培养基为馬血清平衡盐溶液,每毫升接种細胞数为6—10万,于加入药物后24-48小时进行細胞計数,計算药物对細胞生长的抑制百分率,并以形态观察作为輔助指标. 曾进行5种已知抗肿瘤药的敏感試驗,发現药物的作用强度为:氮芥>氧化氮芥>新恩必恨>丁二醇二甲磺酸酯(myleran)>6-巯基嘌呤.此外,过篩了24种合成药和93种天然药物成分,其中有作用者分別为41.7%和38.7%.将篩选結果与动物瘤体內結果作比較,发現二者间有一定的相关.最后对方法的优缺点进行了討論.

5-Alkoxy and 5-substituted phenoxy-2-thiouracils (Ⅳ, Ⅴ), uracils (Ⅵ, Ⅶ), 2-carboxymethyl mercapto-4-hydroxypyrimidines (Ⅷ, Ⅸ) and 2-amino-4-hydroxypyrimidines (Ⅹ) have been synthesized for the investigation of cancer chemotherapy. 5-Substituted thiouracils (Ⅳ, Ⅴ) or 2-amino-4-hydroxy 5-substituted pyrimidines (Ⅷ, Ⅸ) were prepared by the condensation of an appropriate ethyl α-substituted (β-hydroxy acrylate (ⅩⅡ) with thiourea or guanidine. (Ⅳ) or (Ⅴ) reacted with chloroacetic acid in sodium hydroxide solution...

5-Alkoxy and 5-substituted phenoxy-2-thiouracils (Ⅳ, Ⅴ), uracils (Ⅵ, Ⅶ), 2-carboxymethyl mercapto-4-hydroxypyrimidines (Ⅷ, Ⅸ) and 2-amino-4-hydroxypyrimidines (Ⅹ) have been synthesized for the investigation of cancer chemotherapy. 5-Substituted thiouracils (Ⅳ, Ⅴ) or 2-amino-4-hydroxy 5-substituted pyrimidines (Ⅷ, Ⅸ) were prepared by the condensation of an appropriate ethyl α-substituted (β-hydroxy acrylate (ⅩⅡ) with thiourea or guanidine. (Ⅳ) or (Ⅴ) reacted with chloroacetic acid in sodium hydroxide solution to form 2-carboxymethyl mercaptopyrimidines (Ⅷ) or (Ⅸ). After acidifying and refluxing for 3-4 hrs., the corresponding uracils (Ⅵ) or (Ⅶ) were obtained. They could also be prepared directly by treating the appropriate thiouracils (Ⅳ) or (Ⅴ) with Chloroacetic acid. The ethyl a-substituted β-hydroxyacrylate (ⅩⅡ) were prepared by formylating the ethyl alkoxy (or aryloxy) acetate with ethyl formate in the presence of sodium or sodium methoxide. 5-p(or m)-Amino-phenoxy-thiouracil (V_(12)) or (V_(13)) was readily formed when 5-p (or m)-acetamido compound (V_(10)) or (V_(11)) was hydrolyzed with hydrochloric acid. On treating with chloroacetic acid, 5-p(or m)-amino-phenoxy-uracil (Ⅶ_(11)) or (Ⅶ_(12)) was obtained. (Ⅶ_(11)) could also be prepared by hydrogenation of 5-p-nitro-phenoxy-uracil (Ⅶ_(10)), which was prepared by nitration of 5-phenoxy-uracil (Ⅶ_1) or thiouracil (Ⅴ_1). When 5-p-amino-phenoxy thiouracil (V_(11)) was treated first with fluoro-boric acid and sodium nitrite (Schiemann reaction) and then with chloroacetic acid, 5-p-fluorophenoxy uracil (Ⅶ_9) was obtained. An alternative route was carried out through the condensation of an appropriate ethyl α-p (or o, m)-fluoro phenoxy β-hydroxy acrylate with thiourea and then treatment with chloroacetic acid. Hydroxyethylation of the corresponding 5-amino phenoxy uracil (Ⅶ_(11)) or (Ⅶ_(12)) with ethylene oxide, or condensation of the ethyl α-bis (β-hydroxyethyl) amino phenoxy β-hydroxyacrylate with thiourea following with chloroacetic acid treatement, afforded the 5-p (or m)-bis (β-hydroxyethyl) amino phenoxy uracil (Ⅶ_(13)) or (Ⅶ_(13)), from which 5-p-(or m)-bis (β-chloroethyl) aminophenoxy 2,4-dichloro pyrimidine (ⅩⅢ) was prepared by chlorination with phosphorus oxychloride. On hydrolysis of the tetrachloro compounds (ⅩⅢ) with hydrochloric acid, the two new nitrogen mustards-5-p (and m)-bis (β-chloro-ethyl) amino phenoxy uracils were obtained. Preliminary biological test showed that compounds (Ⅳ-1, (Ⅳ-4), (Ⅴ_5), (Ⅴ_6), (Ⅴ_7), (Ⅵ_3), (Ⅶ_8), (Ⅶ_(15)), (Ⅶ_(16)), (Ⅸ_7) and (Ⅹ_1) inhibited the growth of sarcoma 180 in mice.

本文报导了一系列5-烷氧基和5-取代苯氧基硫氧嘧啶(Ⅳ,Ⅴ)、5-烷氧基和5-取代苯氧基尿嘧啶(Ⅵ,Ⅶ)、5-烷氧基-和5-取代苯氧基-4-徑基-2-羧甲硫基嘧啶(Ⅷ,Ⅸ)及5-取代苯氧基-2-氨基-4-羟基嘧啶(Ⅹ)等化合物的合成,以进行抗肿瘤試驗. 初步药理試驗結果显示:化合物(Ⅳ_1),(Ⅳ_4),(Ⅴ_4),(Ⅴ_6),(Ⅴ_7),(Ⅵ_3),(Ⅶ_8),(Ⅶ_(15)),(Ⅶ_(16)),(Ⅸ_7)和(Ⅹ_1)对肉瘤180有明显的抑制作用.

 
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