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lgq101木虫 (小有名气)
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[求助]
求翻译！！！急~~~谢谢
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| We have synthesized a library of 190 polycyclic, alkaloid/terpenoid-like small molecules using solid-phase transition metalmediated cycloaddition and cyclization reactions of relatively simple enyne and diyne substrates. The key sulfinamide lynchpin was also diversified to the corresponding free amines and sulfonamides. Translation to solid-phase synthesis using a TBDAS linker was greatly facilitated by the use of a TBDPS surrogate during earlier solution-phase studies. Principal component analysis of structural and physicochemical parameters indicates that this library samples regions of chemical space that overlap with bona fide natural products and are distinct from those areas accessed by conventional drugs and drug-like libraries. Aromatic ring content and stereochemical complexity were identified as two major factors that distinguish natural products from synthetic drugs. The complete set of 190 compounds is now being screened in a variety of assays at The Rockefeller University High-Throughput Screening Resource Center. In addition, 94 compounds have been submitted for broad screening in the National Institutes of Health (NIH) Molecular Libraries Program . These efforts will provide critical data to evaluate the biological properties of this library and to assess the abilities of natural product-based libraries to address challenging biological targets that remain intractable to conventional drug-like molecules. |
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8814402
至尊木虫 (职业作家)
- 翻译EPI: 509
- 应助: 18 (小学生)
- 贵宾: 0.381
- 金币: 12916.1
- 散金: 47
- 红花: 16
- 帖子: 4183
- 在线: 357.8小时
- 虫号: 1184404
- 注册: 2011-01-06
- 专业: 药物学其他科学问题
【答案】应助回帖
lgq101(金币+30, 翻译EPI+1): 谢谢 2011-06-02 09:55:59
| We have synthesized a library of 190 polycyclic, alkaloid/terpenoid-like small molecules using solid-phase transition metal mediated cycloaddition and cyclization reactions of relatively simple enyne and diyne substrates.我们以相对简单的烯炔和二炔为底物，通过固相过渡金属媒介环加成和环合反应构建了包括190种多环、生物碱/类萜样小分子的文库。 The key sulfinamide lynchpin was also diversified to the corresponding free amines and sulfonamides. 关键的亚磺酰胺也随相应的游离胺和磺酰胺类的不同而多样化。Translation to solid-phase synthesis using a TBDAS linker was greatly facilitated by the use of a TBDPS surrogate during earlier solution-phase studies.使用在先前的液相研究中的TBDPS代用品，促进了利用TBDAS linker实现向固相合成的转换。 Principal component analysis of structural and physicochemical parameters indicates that this library samples regions of chemical space that overlap with bona fide natural products and are distinct from those areas accessed by conventional drugs and drug-like libraries. 结构和物理化学参数的主成分分析标明，这一文库与真实的天然产物在化学空间区域上有重叠，而与由传统的药物或药物样文库获取的区域截然不同。Aromatic ring content and stereochemical complexity were identified as two major factors that distinguish natural products from synthetic drugs. 芳环含量和立体化学复杂度是两个区分天然产物和合成药物的主要因素。The complete set of 190 compounds is now being screened in a variety of assays at The Rockefeller University High-Throughput Screening Resource Center. 整套190种化合物现在在洛克菲勒大学高通量筛选资源中心接受各种各样的筛选试验。In addition, 94 compounds have been submitted for broad screening in the National Institutes of Health (NIH) Molecular Libraries Program . 此外，其中的94种化合物还提交给NIH分子文库项目进行更广泛的筛选。These efforts will provide critical data to evaluate the biological properties of this library and to assess the abilities of natural product-based libraries to address challenging biological targets that remain intractable to conventional drug-like molecules.这些努力将提供必要的数据，以评价这一文库中化合物的生物学性能和评估基于天然产物的文库在应对传统药物样分子无法处理的生物靶标方面的能力。 |
2楼2011-06-02 08:28:00
