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AnnF版主 (文坛精英)
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[求助]
求助翻译一段药物化学方面的英文（英译中），灰常重谢！！！
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1. Introduction Peptides are among the most versatile bioactive molecules e.g.many peptide hormones and analogous short peptides exert their action by binding to membrane receptors [1]. Peptides and their derivatives may also exhibit a broad spectrum of biological activ-ities such as antimicrobial [2], antiviral, and anticancer activities[3]. However, most natural peptides are composed of L -form a-amino acids and because of the ubiquitous prevalence of pepti-dases, they have limited biostability, and consequently low bioavailability. To overcome this problem, stable and at the same time biologically active pseudo-peptides have been developed. These novel compounds open up new perspectives in drug design by providing an entire range of highly speci fi c and non-toxic pharmaceuticals. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have directed considerable attention on the research of pseudo-peptide derivatives mimicking the pharmacophore and thus the activity of the original peptide [4,5]. As isosteres of peptides, phosphono-peptides containing a transition state analogue of the hydrolysis of the amide bond represent another attractive approach for the preparation of proteolytically stable peptides [6]. In addition to increased stability, incorporation of a phosphonate moiety into the peptide sequence also provides access to additional binding interactions within the transition state conformation of the enzyme/substrate complex [7]. A wide range of phosphonopep-tides have been used to design very effective protease inhibitors[8 -10 ]. However, since there are only a limited number of economically viable chemicals available for practical application in biological science or agriculture [11] , a great deal of scope still lies ahead for further research in this field. In this context, in order to find broad spectrum biologically active pseudo-peptide thiourea, we have previously described preparation of certain chiral thio-urea derivatives containing a-aminophosphonate moiety with signifi cant antiviral activity [12]. Herein, we further turned our attention to prepare novel compounds with enhanced antitumor activities by incorporating a-aminophosphonate moiety at the 1 or 3-position of pseudo-peptide thiourea. The primary aim of this study is to synthesize the title compounds and study their anti-tumor activities for the development of a new inhibitor to PC3, Bcap37 and BGC823 cells. To the best of our knowledge, this is the first report on the synthesis and antitumor activity of pseudo-peptide thioureas containing a-aminophosphonate moiety.  英文原文.png [ Last edited by AnnF on 2012-12-29 at 17:30 ] |
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爱与雨下: 金币+2 2012-12-29 20:53:27
AnnF: 金币+5, 翻译EPI+1, ★有帮助, 希望有更准确的译文，O(∩_∩)O谢谢！ 2012-12-29 22:34:44
爱与雨下: 金币+2 2012-12-29 20:53:27
AnnF: 金币+5, 翻译EPI+1, ★有帮助, 希望有更准确的译文，O(∩_∩)O谢谢！ 2012-12-29 22:34:44
| 肽是最通用的生物活性分子，例如许多肽类激素和通过核膜受体结合类似的短肽 [ 1 ]。肽及其衍生物也可能表现出广泛的生物活性等例如抗菌，抗病毒，抗癌活性等。然而，最自然的多肽是由L-α-氨基酸，因为无处不在的流行肽酶生物稳定定性有限，因此生物利用度低。为了克服这个问题，已开发了稳定并且同时具有生物活性的伪肽。 这些新化合物开辟了新的前景药物设计并为其提供了一整套非常明确的和无毒的药物。 随着越来越多的应用的合成和生物活性，化学家和生物学家最近几年在研究伪肽衍生物的药效相当重视，从而模仿活性的原始肽[ 4 , 5 ]。 作为电子等排物肽，氨基磷酸肽含有过渡态类似物水解酰胺结合是另一个有吸引力的方法，能够用于制备蛋白水解稳定肽[ 6 ]。 除了能增加稳定性外，在过渡态构象的酶/底物中，一部分的多肽序列能提供额外的约束力的。范围广泛的氨基磷酸肽已用于设计非常有效的蛋白酶抑制剂[ 8 - 10 ]。 然而，由于只有有限数量的经济上可行的化学品可用于实际应用生物科学或农业[ 11 ]，大范围的应用仍需要进一步研究。在这方面，为了寻找广谱生物活性的伪肽硫脲，之前我们已经研究制备某些手性硫脲（用于治疗甲亢、照相术等） 衍生物含有A-氨基膦酸酯基团成分具有显著的抗病毒活性[ 12 ]。 在此，我们进一步研究了在1或3位伪肽硫脲具有增强抗肿瘤活性结合A-氨基膦酸酯基团成分的新的化合物。这项研究的主要目的是合成标题化合物，并研究能在前列腺癌，bcap37和BGC 823细胞中使具有其抗肿瘤活性并能开发新的抑制剂。据我们所知，这是首次报告了含有A-氨基膦酸酯硫脲基团合成和抗肿瘤活性的伪肽。 |
2楼2012-12-29 18:54:25
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