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lgq101木蟲(chóng) (小有名氣)
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[求助]
求翻譯�。�！急~~~謝謝
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| Alkaloid and terpenoid natural products display an extensive array of chemical frameworks and biological activities. However such scaffolds remain underrepresented in current screening collections and are, thus, attractive targets for the synthesis of natural product-based libraries that access underexploited regions of chemical space. Recently, we reported a systematic approach to the stereoselective synthesis of multiple alkaloid/terpenoid-like scaffolds using transition metal-mediated cycloaddition and cyclization reactions of enyne and diyne substrates assembled on a tert-butylsulfinamide lynchpin. We report herein the synthesis of a 190-membered library of alkaloid/terpenoid-like molecules using this synthetic approach. Translation to solid-phase synthesis was facilitated by the use of a tert-butyldiarylsilyl (TBDAS) linker that closely mimics the tert-butyldiphenysilyl protecting group used in the original solution-phase route development work. Unexpected differences in stereoselectivity and regioselectivity were observed in some reactions when carried out on solid support. Further, the sulfinamide moiety could be hydrolyzed or oxidized efficiently without compromising the TBDAS linker to provide additional amine and sulfonamide functionalities. Principal component analysis of the structural and physicochemical properties of these molecules confirmed that they access regions of chemical space that overlap with bona fide natural products and are distinct from areas addressed by conventional synthetic drugs and drug-like molecules. The influences of scaffolds and substituents were also evaluated, with both found to have significant impacts on location in chemical space and three-dimensional shape. Broad biological evaluation of this library will provide valuable insights into the abilities of natural product-based libraries to access similarly underexploited regions of biological space. |
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【考研調(diào)劑】化學(xué)專(zhuān)業(yè) 281分，一志愿四川大學(xué)，誠(chéng)心求調(diào)劑
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zuodg
鐵桿木蟲(chóng) (正式寫(xiě)手)
有為青年
- 翻譯EPI: 180
- 應(yīng)助: 5 (幼兒園)
- 貴賓: 0.015
- 金幣: 6765.2
- 散金: 48
- 紅花: 18
- 帖子: 500
- 在線(xiàn): 285.5小時(shí)
- 蟲(chóng)號(hào): 1055187
- 注冊(cè): 2010-07-10
- 性別: GG
- 專(zhuān)業(yè): 外國(guó)語(yǔ)言
【答案】應(yīng)助回帖
★
sltmac(金幣+1): 謝謝應(yīng)助~~ 2011-05-31 15:26:31
lgq101(金幣+40, 翻譯EPI+1): 謝謝 2011-05-31 21:17:58
sltmac(金幣+1): 謝謝應(yīng)助~~ 2011-05-31 15:26:31
lgq101(金幣+40, 翻譯EPI+1): 謝謝 2011-05-31 21:17:58
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生物堿和萜類(lèi)天然產(chǎn)物具有一些列豐富的化學(xué)結(jié)構(gòu)和生物活性。 然而目前這些結(jié)構(gòu)骨架在篩選時(shí)還沒(méi)有受到足夠的重視，因此是化學(xué)合成天然產(chǎn)物文庫(kù)、探索未知化學(xué)空間的魅力靶標(biāo)。 最近，我們報(bào)道了一個(gè)使用過(guò)渡態(tài)金屬介導(dǎo)炔、二炔底物（裝配在t-丁基磺胺上）環(huán)加成與環(huán)化、通過(guò)立體化學(xué)系統(tǒng)合成多個(gè)生物堿/萜類(lèi)結(jié)構(gòu)骨架的研究。使用該合成方法我們合成一個(gè)包含190種化合物的生物堿/萜類(lèi)化合物文庫(kù)。固態(tài)合成借助于TBDAS鏈接分子（該分子與液態(tài)合成所用的t-丁基磺胺保護(hù)集團(tuán)很類(lèi)似）。固態(tài)合成發(fā)現(xiàn)有些反應(yīng)的立體選擇性與區(qū)位選擇性不相同。此外，磺胺基團(tuán)會(huì)發(fā)生高效水解或氧化，不能繼續(xù)提供胺基與磺胺基。對(duì)文庫(kù)分子的結(jié)構(gòu)性質(zhì)與理化性質(zhì)進(jìn)行分析發(fā)現(xiàn)， 這些分子的化學(xué)空間與天然產(chǎn)物有重疊，與傳統(tǒng)合成藥物或藥物類(lèi)似物分子的化學(xué)空間不同�；瘜W(xué)結(jié)構(gòu)骨架與取代基的影響也進(jìn)行了評(píng)估，發(fā)現(xiàn)對(duì)化學(xué)空間的定位與三級(jí)結(jié)構(gòu)有顯著影響。文庫(kù)生物活性的評(píng)估對(duì)于基于天然產(chǎn)物的文庫(kù)探索未探索生物空間具有重要價(jià)值。 |
2樓2011-05-31 13:34:09
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