Application of Glaser-Hay Diyne Coupling To Constrain Nα-Amino Acid Amides via a N-N Bridge [0.03%]
Glaser-Hay偶联反应通过N-N桥限制Nα氨基酸酰胺的构象异构体的研究
Sergii Okorochenkov,Viktor Krchňák
Sergii Okorochenkov
We present the application of a Glaser-Hay diyne coupling for the synthesis of conformationally constrained Nα-amino acid amides with different diyne ring sizes. Twelve-membered rings were the smallest rings that could be prepared by this ...
Quantitative Comparison of Enrichment from DNA-Encoded Chemical Library Selections [0.03%]
DNA编码化学文库筛选的富集定量比较
John C Faver,Kevin Riehle,David R Lancia Jr et al.
John C Faver et al.
DNA-encoded chemical libraries (DELs) provide a high-throughput and cost-effective route for screening billions of unique molecules for binding affinity for diverse protein targets. Identifying candidate compounds from these libraries invol...
Comparative Study
ACS combinatorial science. 2019 Feb 11;21(2):75-82. DOI:10.1021/acscombsci.8b00116 2019
Synthesis of Aza-acyclic Nucleoside Libraries of Purine, Pyrimidine, and 1,2,4-Triazole [0.03%]
嘌呤、嘧啶和1,2,4-三氮唑类aza-亚环核苷库的合成
Vibha Pathak,Ashish K Pathak,Robert C Reynolds
Vibha Pathak
Under the aegis of the Pilot Scale Library Program of the NIH Roadmap Initiative, a new library of propan-1-amine containing aza acyclic nucleosides was designed and prepared, and we now report a diverse set of 157 purine, pyrimidine, and 1...
Highly Regioselective, Acid-Catalyzed, Three-Component Cascade Reaction for the Synthesis of 2-aminopyridine-Decorated Imidazo[1,2- a]pyridine [0.03%]
一种合成2-氨基吡啶修饰的imidazo[1,2-a]吡啶的高度区域选择性酸催化三组分级联反应
Qiu-Xing He,Yao-Feng Liang,Chang Xu et al.
Qiu-Xing He et al.
A highly regioselective acid-catalyzed three-component reaction of 2-aminopyridine and 3-phenylpropiolaldehyde for the construction of imidazo[1,2- a]pyridine has been developed. This strategy provides a broad range of substrates and repres...
Rajendra V Patil,Jagdish U Chavan,Dipak S Dalal et al.
Rajendra V Patil et al.
The Biginelli product, dihydropyrimidinone (DHPM) core, and its derivatives are of immense biological importance. There are several methods reported as modifications to the original Biginelli reaction. Among them, many involve the use of di...
Petra Králová,Sandra Benická,Miroslav Soural
Petra Králová
The synthesis of different diketomorpholines via N-acyl-3,4-dihydro-2 H-1,4-oxazine-3-carboxylic acids is reported in this article. The key intermediates were prepared using a convenient solid-phase synthesis starting from polymer-supported...
Syamak Farajikhah,Joan M Cabot,Peter C Innis et al.
Syamak Farajikhah et al.
Novel approaches that incorporate electrofluidic and microfluidic technologies are reviewed to illustrate the translation of traditional enclosed structures into open and accessible textile based platforms. Through the utilization of on-fib...
Targeting Protein-Protein Interactions of Tyrosine Phosphatases with Microarrayed Fragment Libraries Displayed on Phosphopeptide Substrate Scaffolds [0.03%]
基于微阵列的肽片段文库筛选磷酸肽底物支架上的酪氨酸磷酸酶相互作用蛋白
Megan Hogan,Medhanit Bahta,Kohei Tsuji et al.
Megan Hogan et al.
Chemical library screening approaches that focus exclusively on catalytic events may overlook unique effects of protein-protein interactions that can be exploited for development of specific inhibitors. Phosphotyrosyl (pTyr) residues embedd...
Bicyclic RGD Peptides with Exquisite Selectivity for the Integrin αvβ3 Receptor Using a "Random Design" Approach [0.03%]
利用“随机设计”方法获得的具有高精密度αvβ3受体选择性的双环RGD肽类分子
Dominik Bernhagen,Vanessa Jungbluth,Nestor Gisbert Quilis et al.
Dominik Bernhagen et al.
We describe the identification of bicyclic RGD peptides with high affinity and selectivity for integrin αvβ3 via high-throughput screening of partially randomized libraries. Peptide libraries (672 different compounds) comprising the unive...
Cellular-Based Selections Aid Yeast-Display Discovery of Genuine Cell-Binding Ligands: Targeting Oncology Vascular Biomarker CD276 [0.03%]
基于蜂群的筛选助力酵母展示发现真正的细胞结合配体：靶向肿瘤血管生物标志物CD276
Lawrence A Stern,Patrick S Lown,Alexandra C Kobe et al.
Lawrence A Stern et al.
Yeast surface display is a proven tool for the selection and evolution of ligands with novel binding activity. Selections from yeast surface display libraries against transmembrane targets are generally carried out using recombinant soluble...