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北京石油化工學(xué)院2026年研究生招生接收調(diào)劑公告

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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.

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[ Last edited by AnnF on 2012-12-29 at 17:30 ]

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1樓 2012-12-29 17:24:30

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愛與雨下: 金幣+2 2012-12-29 20:53:27
AnnF: 金幣+5, 翻譯EPI+1, ★有幫助, 希望有更準(zhǔn)確的譯文，O(∩_∩)O謝謝！ 2012-12-29 22:34:44

肽是最通用的生物活性分子，例如許多肽類激素和通過核膜受體結(jié)合類似的短肽 [ 1 ]。肽及其衍生物也可能表現(xiàn)出廣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，因為無處不在的流行肽酶生物穩(wěn)定定性有限，因此生物利用度低。為了克服這個問題，已開發(fā)了穩(wěn)定并且同時具有生物活性的偽肽。這些新化合物開辟了新的前景藥物設(shè)計并為其提供了一整套非常明確的和無毒的藥物。隨著越來越多的應(yīng)用的合成和生物活性，化學(xué)家和生物學(xué)家最近幾年在研究偽肽衍生物的藥效相當(dāng)重視，從而模仿活性的原始肽[ 4 , 5 ]。作為電子等排物肽，氨基磷酸肽含有過渡態(tài)類似物水解酰胺結(jié)合是另一個有吸引力的方法，能夠用于制備蛋白水解穩(wěn)定肽[ 6 ]。除了能增加穩(wěn)定性外，在過渡態(tài)構(gòu)象的酶/底物中，一部分的多肽序列能提供額外的約束力的。范圍廣泛的氨基磷酸肽已用于設(shè)計非常有效的蛋白酶抑制劑[ 8 - 10 ]。然而，由于只有有限數(shù)量的經(jīng)濟(jì)上可行的化學(xué)品可用于實際應(yīng)用生物科學(xué)或農(nóng)業(yè)[ 11 ]，大范圍的應(yīng)用仍需要進(jìn)一步研究。在這方面，為了尋找廣譜生物活性的偽肽硫脲，之前我們已經(jīng)研究制備某些手性硫脲（用于治療甲亢、照相術(shù)等）衍生物含有A-氨基膦酸酯基團(tuán)成分具有顯著的抗病毒活性[ 12 ]。在此，我們進(jìn)一步研究了在1或3位偽肽硫脲具有增強(qiáng)抗腫瘤活性結(jié)合A-氨基膦酸酯基團(tuán)成分的新的化合物。這項研究的主要目的是合成標(biāo)題化合物，并研究能在前列腺癌，bcap37和BGC 823細(xì)胞中使具有其抗腫瘤活性并能開發(fā)新的抑制劑。據(jù)我們所知，這是首次報告了含有A-氨基膦酸酯硫脲基團(tuán)合成和抗腫瘤活性的偽肽。

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2樓2012-12-29 18:54:25

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