Journal ArticleDOI
Visible Light-Promoted Divergent Benzoheterocyclization from Aldehydes for DNA-Encoded Chemical Libraries.
TLDR
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.About:
This article is published in Organic Letters.The article was published on 2022-04-25. It has received 14 citations till now. The article focuses on the topics: Medicine & Chemistry.read more
Citations
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Journal ArticleDOI
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
Aryl diazonium intermediates enable mild DNA-compatible C–C bond formation for medicinally relevant combinatorial library synthesis
TL;DR: Forging carbon-carbon linkage in DNA-encoded combinatorial library synthesis represents a fundamental task for drug discovery, especially with broad substrate scope and exquisite functional group tolerance.
Journal ArticleDOI
On-DNA Synthesis of Functionalized 4H-Pyran Scaffolds for Focused DNA-Encoded Chemical Libraries.
TL;DR: The functionalized 4H-pyran scaffold is disclosed, combining this scaffold with the merits of scaffold architecture in drug design, and open the door for the construction of DNA-encoded chemical libraries with more consideration for this structural architecture.
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.
References
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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
Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines.
Catriona G. Mortimer,Geoffrey Wells,Jean-Philippe Crochard,Erica L. Stone,Tracey D. Bradshaw,Malcolm F. G. Stevens,Andrew D. Westwell +6 more
TL;DR: Mechanistically, this new series of agents contrasts with the previously reported 2-(4-aminophenyl)benzothiazoles; compound 8n is not reliant on induction of CYP1A1 expression for antitumor activity.
Journal ArticleDOI
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Sarah Picaud,Christopher Wells,I. Felletar,Deborah Brotherton,Sarah Martin,Pavel Savitsky,Beatriz Diez-Dacal,Martin Philpott,C. Bountra,Hannah Lingard,Oleg Fedorov,Susanne Müller,Paul Brennan,Stefan Knapp,Panagis Filippakopoulos +14 more
TL;DR: The discovery and characterization of RVX-208 as a domain-selective inhibitor of BETs and a potential mechanism of action of a clinical compound that was identified based on phenotypic screens are reported and demonstrated.
Journal ArticleDOI
A biomolecule-compatible visible-light-induced azide reduction from a DNA-encoded reaction-discovery system
TL;DR: Reactionivity that led to a biomolecule-compatible, Ru(II)-catalyzed, visible light-induced azide reduction reaction, which provides a means of photouncaging functional groups such as amines and carboxylates on biological macromolecules without using UV irradiation.
Journal ArticleDOI
Open-Air Alkylation Reactions in Photoredox-Catalyzed DNA-Encoded Library Synthesis.
James P. Phelan,Simon B. Lang,Jaehoon Sim,Simon Berritt,Andrew J. Peat,Katelyn Billings,Lijun Fan,Gary A. Molander +7 more
TL;DR: DNA-encoded library technology is a powerful tool commonly used by the pharmaceutical industry for the identification of compounds with affinity to biomolecular targets by merging Ni/photoredox dual catalytic C(sp2)-C(sp3) cross-coupling as well as photoredox-catalyzed radical/polar crossover alkylation protocols with DELs.