Journal ArticleDOI
Diversity-oriented synthesis as a tool to expand the chemical space of DNA-encoded libraries.
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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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Vinyl azide as a synthon for DNA-compatible divergent transformations into N-heterocycles.
TL;DR: A series of DNA-compatible transformations utilizing on-DNA vinyl azide as a synthon to forge divergent N-heterocyclic scaffolds are developed to demonstrate the feasibility of these N- heterocycle syntheses in DNA-encoded chemical library construction.
Journal ArticleDOI
Development of on-DNA vinyl sulfone synthesis for DNA-encoded chemical libraries
Yangfeng Li,Yizhou Li +1 more
TL;DR: In this paper , the development of an efficient synthetic route to generate a DNA-compatible vinyl sulfone functional group, and subsequent chemical transformations demonstrated the feasibility of their method in DEL construction.
Journal ArticleDOI
Antimony salt-promoted cyclization facilitating on-DNA syntheses of dihydroquinazolinone derivatives and its applications
TL;DR: In this article , a facile synthesis of on-DNA dihydroquinazolinone from aldehyde and anthranilamide was reported, which was promoted by antimony trichloride, which has proven to accelerate the reaction and improve conversions.
Journal ArticleDOI
Recent ring distortion reactions for diversifying complex natural products.
TL;DR: This work reviews the ring distortion reactions recently used in complexity-to-diversity (CtD) and pseudo natural products (pseudo-NPs) strategies for diversifying complex natural products and provides a toolbox for chemists for the application of ring distort reactions to access natural product-like molecules.
Journal ArticleDOI
Alkyne Activation in the Diversity Oriented Synthesis of sp2‐Rich Scaffolds: A Biased Library Approach for Targeting Polynucleotides (DNA/RNA)
Shuqi Chen,Daniel L. Priebbenow,Julie Somkhit,Carmen V. Scullino,Keli Agama,Yves Pommier,Bernard L. Flynn +6 more
TL;DR: To assist in designing a polynucleotide-biased library, a scaffold-divergent synthesis approach to polyfused aromatic scaffolds has been undertaken, generating a novel TOP1 inhibitory chemotype.
References
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Journal ArticleDOI
Photoredox Catalysis in Organic Chemistry
TL;DR: This Perspective highlights the unique ability of photoredox catalysis to expedite the development of completely new reaction mechanisms, with particular emphasis placed on multicatalytic strategies that enable the construction of challenging carbon-carbon and carbon-heteroatom bonds.
Journal ArticleDOI
Encoded combinatorial chemistry.
Sydney Brenner,Richard A. Lerner +1 more
TL;DR: The diversity of chemical synthesis and the power of genetics are linked to provide a powerful, versatile method for drug screening that can be amplified by replication and utilized for enrichment of the bound molecules by serial hybridization to a subset of the library.
Journal ArticleDOI
Design, synthesis and selection of DNA-encoded small-molecule libraries
Matthew A. Clark,Raksha A. Acharya,Christopher C. Arico-Muendel,Svetlana L. Belyanskaya,Dennis Benjamin,Neil R Carlson,Paolo A. Centrella,Cynthia H. Chiu,Steffen Phillip Creaser,John W. Cuozzo,Christopher P. Davie,Yun Ding,G Joseph Franklin,Kurt D Franzen,Malcolm L. Gefter,Steven P Hale,Nils Jakob Vest Hansen,David I. Israel,Jinwei Jiang,Malcolm J. Kavarana,Michael Kelley,Christopher S. Kollmann,Fan Li,Kenneth E Lind,Sibongile Mataruse,Patricia F Medeiros,Jeffrey A. Messer,Paul Myers,Heather O’Keefe,Matthew C Oliff,Cecil E Rise,Alexander L. Satz,Steven R. Skinner,Jennifer L Svendsen,Lujia Tang,Kurt van Vloten,Richard W. Wagner,Gang Yao,Baoguang Zhao,Barry A. Morgan +39 more
TL;DR: An 800-million-member DNA-encoded library in which small molecules are covalently attached to an encoding oligonucleotide is reported, assembled by a combination of chemical and enzymatic synthesis, and interrogated by affinity selection.
Journal ArticleDOI
DNA-templated organic synthesis: nature's strategy for controlling chemical reactivity applied to synthetic molecules.
Xiaoyu Li,David R. Liu +1 more
TL;DR: DNA-templated organic synthesis (DTS) is emerging as a surprisingly general way to control the reactivity of synthetic molecules by using nature's effective-molarity-based approach.
Journal ArticleDOI
Towards the Optimal Screening Collection: A Synthesis Strategy
TL;DR: A newly emerging strategy in diversity-oriented small-molecule synthesis that may have the potential to achieve challenging goals in synthetic chemistry is reviewed.