Journal ArticleDOI
Diversity-oriented synthesis as a tool to expand the chemical space of DNA-encoded libraries.
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TLDR
In this paper, a review of DNA-compatible complexity-generating reactions that can be applied for the generation of DNAencoded DOS libraries, including: (i) multicomponent reactions; (ii) C-H/C-X functionalization; (iii) tandem approaches; (iv) cycloadditions; (v) reactions introducing privileged elements.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2021-05-15. It has received 12 citations till now. The article focuses on the topics: Chemical space.read more
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Journal ArticleDOI
Strategies for developing DNA-encoded libraries beyond binding assays
Yiran Huang,Yizhou Li,Xiaoyu Li +2 more
TL;DR: The recent progress in using DNA-encoded chemical libraries to interrogate complex biological targets and their potential to identify structures that elicit function or possess other useful properties are discussed.
Journal ArticleDOI
Visible Light-Promoted Divergent Benzoheterocyclization from Aldehydes for DNA-Encoded Chemical Libraries.
TL;DR: A visible light-promoted divergent synthesis of on-DNA benzoheterocycles from aldehydes is presented, demonstrating the feasibility of this approach in DNA-encoded chemical library construction.
Journal ArticleDOI
Sequential DNA-Encoded Building Block Fusion for the Construction of Polysubstituted Pyrazoline Core Libraries.
TL;DR: A sequential DNA-encoded synthesis strategy for polysubstituted pyrazoline heterocycles, which fuses a broad panel of aldehydes, aryl amines, and alkenes as building blocks, was presented in this paper.
Journal ArticleDOI
Converting Double-Stranded DNA-Encoded Libraries (DELs) to Single-Stranded Libraries for More Versatile Selections
TL;DR: It is shown that dsD ELs could be efficiently converted to ssDELs and used for affinity-based selections either with purified proteins or on live cells.
Journal ArticleDOI
Recent advances in DNA-encoded dynamic libraries
Bingbing Shi,Yu Zhou,Xiaoyu Li +2 more
TL;DR: The DNA-encoded dynamic combinatorial libraries (DCLs) as mentioned in this paper have been widely adopted in the pharmaceutical industry and a number of clinical drug candidates have been identified from DEL selections.
References
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Journal ArticleDOI
Aminoazole-Based Diversity-Oriented Synthesis of Heterocycles.
Maryna V. Murlykina,Alisa D. Morozova,Ievgen M. Zviagin,Yana I. Sakhno,Sergey M. Desenko,Sergey M. Desenko,Valentyn A. Chebanov,Valentyn A. Chebanov +7 more
TL;DR: The comprehensive review contains the analysis of literature data concerning reactions of heterocyclization of aminoazoles and demonstrates the application of these types of transformations in diversity-oriented synthesis.
Journal ArticleDOI
Merging C(sp3)–H activation with DNA-encoding
Zhoulong Fan,Shuai Zhao,Tao Liu,Peng-Xiang Shen,Zi-Ning Cui,Zhe Zhuang,Qian Shao,Jason S. Chen,Anokha S. Ratnayake,Mark Edward Flanagan,Dominik K. Kölmel,David W. Piotrowski,Paul G. Richardson,Jin-Quan Yu +13 more
TL;DR: P palladium-catalyzed C(sp3)–H arylation of aliphatic carboxylic acids, amides and ketones with DNA-encoded aryl iodides in water enables the use of alternative sets of monofunctional building blocks, providing a linchpin to facilitate further setup for DELs.
Journal ArticleDOI
Water-Compatible Cycloadditions of Oligonucleotide-Conjugated Strained Allenes for DNA-Encoded Library Synthesis.
Matthias V Westphal,Liam Hudson,Liam Hudson,Jeremy W Mason,Jeremy W Mason,Johan A Pradeilles,Johan A Pradeilles,Frédéric Zecri,Karin Briner,Stuart L. Schreiber,Stuart L. Schreiber +10 more
TL;DR: Strain-promoted cycloadditions of cyclic allenes under mild condi-tions to DNA-encoded library synthesis are introduced and the resulting DNA-barcoded compounds exhibit unprecedented ring and topographic features-related to elements found to be powerful in phenotypic screening.
Journal ArticleDOI
Efficient copper-catalyzed amination of DNA-conjugated aryl iodides under mild aqueous conditions.
Yves Ruff,Frederic Berst +1 more
TL;DR: This protocol leverages a novel ligand, 2-((2,6-dimethoxyphenyl)amino)-2-oxoacetic acid, to effect the transformation in aqueous DMSO, under mild conditions and in air, making it an ideal candidate for the synthesis of DNA-encoded libraries.
Journal ArticleDOI
The state of the art of chemical biology.
Karl-Heinz Altmann,Buchner J,Horst Kessler,François Diederich,Bernhard Kräutler,Stephen J. Lippard,Rob M. J. Liskamp,Klaus Müller,Elizabeth M. Nolan,Bruno Samorì,Gisbert Schneider,Sandra Schreiber,Harald Schwalbe,Claudio Toniolo,van Boeckel Ca,Herbert Waldmann,Christopher T. Walsh +16 more