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
Relay Catalytic Branching Cascade: A Technique to Access Diverse Molecular Scaffolds
TL;DR: Diversity-oriented synthesis (DOS), a terminology ini-tially coined by Schreiber, makes chemical synthesis the only alternative to obtain unambiguously characterized, diverse, multifunctionalmoleculesthataresimilartonaturalproducts.
Journal ArticleDOI
DNA-Encoded Libraries: Aryl Fluorosulfonates as Versatile Electrophiles Enabling Facile On-DNA Suzuki, Sonogashira, and Buchwald Reactions
Hongtao Xu,Fei Ma,Nan Wang,Wei Hou,Huan Xiong,Fengping Lu,Jie Li,Shuyue Wang,Peixiang Ma,Guang Yang,Richard A. Lerner +10 more
TL;DR: Using (hetero)aryl fluorosulfonates as versatile electrophiles, facile on‐DNA cross‐coupling reactions of Suzuki, Sonogashira, and Buchwald are reported here and are highly amenable to synthesis of DNA‐encoded libraries with great molecular diversity.
Journal ArticleDOI
Diversity Oriented Clicking (DOC): Divergent Synthesis of SuFExable Pharmacophores from 2‐Substituted‐Alkynyl‐1‐Sulfonyl Fluoride (SASF) Hubs
Christopher J. Smedley,Gencheng Li,Andrew S. Barrow,Timothy L Gialelis,Marie-Claire Giel,Alessandra Ottonello,Yunfei Cheng,Seiya Kitamura,Dennis W. Wolan,K. Barry Sharpless,John E. Moses,John E. Moses +11 more
TL;DR: This work showcases 2- S ubstituted- A lkynyl-1- S ulfonyl F luorides (SASFs) as a new class of connective hub in concert with a diverse selection of click-cycloaddition processes and reports a diverse click-library of 173 unique functional molecules in minimal synthetic steps.
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Isoquinoline Alkaloids and Their Antiviral, Antibacterial, and Antifungal Activities and Structure-activity Relationship
Journal ArticleDOI
Future challenges with DNA-encoded chemical libraries in the drug discovery domain
TL;DR: The key to the future success of DELs as true discovery modalities, rather than just ‘a way to make many compounds,’ is to go beyond physical binding to functional or even phenotypic assays with the capability to probe the biological system.