Rational Molecular Editing: A New Paradigm in Drug Discovery

Journal of Medicinal Chemistry, Год журнала: 2024, Номер 67(14), С. 11459 - 11466

Опубликована: Июнь 21, 2024

ADVERTISEMENT RETURN TO ARTICLES ASAPPREVEditorialNEXTRational Molecular Editing: A New Paradigm in Drug DiscoveryChunhua MaChunhua MaState Key Laboratory of Antiviral Drugs, Pingyuan Laboratory, NMPA for Research and Evaluation Innovative Drug, School Chemistry Chemical Engineering, Henan Normal University, Xinxiang, 453007, ChinaMore by Chunhua Mahttps://orcid.org/0000-0001-7613-6471, Craig W. Lindsley*Craig LindsleyVanderbilt University Medical Center, Franklin, Tennessee 37027, United States*E-mail: [email protected]More Lindsleyhttps://orcid.org/0000-0003-0168-1445, Junbiao Chang*Junbiao ChangCollege Chemistry, State Zhengzhou 450001, China*E-mail: Chang, Bin Yu*Bin YuCollege Yuhttps://orcid.org/0000-0002-7207-643XCite this: J. Med. Chem. 2024, XXXX, XXX, XXX-XXXPublication Date (Web):June 21, 2024Publication History Received13 June 2024Published online21 2024https://pubs.acs.org/doi/10.1021/acs.jmedchem.4c01347https://doi.org/10.1021/acs.jmedchem.4c01347editorialACS PublicationsPublished 2024 American Society. This publication is available under these Terms Use. Request reuse permissions free to access through this site. Learn MoreArticle Views-Altmetric-Citations-LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum full text article downloads since November 2008 (both PDF HTML) across all institutions individuals. These metrics regularly updated reflect usage leading up last few days.Citations number other articles citing article, calculated Crossref daily. Find more information about citation counts.The Altmetric Attention Score a quantitative measure attention that research has received online. Clicking on donut icon will load page at altmetric.com with additional details score social media presence given article. how calculated. Share Add toView InAdd Full Text ReferenceAdd Description ExportRISCitationCitation abstractCitation referencesMore Options onFacebookTwitterWechatLinked InRedditEmail (2 MB) Get e-AlertscloseSUBJECTS:Drug discovery,Macrocyclization,Molecules,Pharmaceuticals,Scaffolds e-Alerts

Язык: Английский

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Decatungstate-photocatalyzed direct acylation of N-heterocycles with aldehydes

Green Chemistry, Год журнала: 2024, Номер 26(12), С. 7331 - 7336

Опубликована: Янв. 1, 2024

A novel photocatalytic acylation strategy was developed harnessing tetrabutylammonium decatungstate (TBADT) as a hydrogen atom transfer (HAT) photocatalyst to facilitate the direct coupling of aldehydes with N-heterocycles at ambient temperature.

Язык: Английский

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Phototriggered Self-Catalyzed Phosphorylation of 3,4-Dihydroquinoxalin-2(1H)-ones with Diarylphosphine Oxides in EtOH

The Journal of Organic Chemistry, Год журнала: 2024, Номер unknown

Опубликована: Сен. 19, 2024

A highly effective external photocatalyst- and additive-free method for the phosphorylation of 3,4-dihydroquinoxalin-2(1

Язык: Английский

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Direct C–H Alkylation of Benzothiadiazoles via Organic Photoredox Catalysis

The Journal of Organic Chemistry, Год журнала: 2024, Номер 89(4), С. 2777 - 2781

Опубликована: Фев. 5, 2024

2,1,3-Benzothiadiazole is widely used as a privileged scaffold in pharmaceuticals and organic functional materials. Nonetheless, many current methods for the functionalization of 2,1,3-benzothiadiazole rely on preactivation, transition metal catalysts/promoters, or an elevated reaction temperature. Herein we disclose transition-metal-free visible-light-induced photocatalytic method direct C–H alkylation using readily accessible carboxylic acid derivatives, i.e., N-hydroxyphthalimide esters (NHPEs), alkylating reagents under room This mild scalable highlighted by late-stage installation benzothiadiazole drugs natural products.

Язык: Английский

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N-Phenylphenothiazine-based Hyper-cross-linked Polymers for Recyclable, Heterogeneous Photocatalysis of Organic Transformations: A Strategy to Access 6-Difluoromethyl-phenanthridines

Organic Letters, Год журнала: 2025, Номер unknown

Опубликована: Янв. 23, 2025

Herein, a N-phenylphenothiazine-based hyper-cross-linked polymer (PTH-HCP) was finely designed and constructed, which serves as metal-free heterogeneous photocatalyst for organic transformations. Characterization experiments have shown that this demonstrates outstanding stability, extensive surface area, exceptional photoelectric response properties. Moreover, PTH-HCP showed good catalytic efficiency recyclability in the photochemically driven difluoromethylation/cyclization reactions. This work provides strategy design construction of photocatalysts offers support their broad prospects synthetic applications.

Язык: Английский

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TEMPO/O₂ Synergistically Mediated BiBrO‐Photocatalyzed Decarboxylative Phosphorylation of N‐Arylglycines

Chemistry - A European Journal, Год журнала: 2024, Номер 30(41)

Опубликована: Апрель 22, 2024

With both TEMPO and O

Язык: Английский

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Functionalization of 1,3‐Butadiene Derivatives under Photo/Electrocatalysis

European Journal of Organic Chemistry, Год журнала: 2024, Номер 27(28)

Опубликована: Май 20, 2024

Abstract In recent years, the functionalization of 1,3‐butadiene has become an attractive strategy for constructing allyl compounds with molecular and structural complexity, current research focuses on synthetic chemistry organic synthesis. Compared traditional synthesis method, methods promoted by photochemistry or electrochemistry represent environmentally friendly mild strategy. this review, reactions under photochemical/electrochemical processes in years are reviewed according to classification systems, particular emphasis corresponding reaction mechanism, which lays a foundation further exploration new catalytic methods.

Язык: Английский

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Photomediated Hydro(deutero)acylation of Olefins by Decarboxylative Addition of α-Oxocarboxylic Acids

The Journal of Organic Chemistry, Год журнала: 2024, Номер 89(4), С. 2741 - 2747

Опубликована: Фев. 1, 2024

Acyl radicals have been generated from the decarboxylation of α-oxocarboxylic acids by using a readily accessible organic pyrimidopteridine photoredox catalyst under ultraviolet-A (UV-A) light irradiation. These reactive acyl were smoothly added to olefins such as styrenes and diverse Michael acceptors, with assistance H2O/D2O hydrogen donors, enabling easy access range ketones/β-deuterio ketones. A wide are compatible this reaction, which shows reliable, atom-economical, eco-friendly protocol. Furthermore, postsynthetic diversifications applications presented.

Язык: Английский

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Annulation Cascades of Cyclosulfonium Salts and Alkenes towards Sulfur‐Containing N‐Heterocycles by Visible Light/Copper Catalysis

Chinese Journal of Chemistry, Год журнала: 2024, Номер 42(14), С. 1637 - 1643

Опубликована: Апрель 3, 2024

Comprehensive Summary Although, great achievements have been made in the synthesis of heterocycles using radical addition/cyclization strategy, developing versatile alkyl precursors, especially non‐stabilized long chain radicals for this strategy still remains a huge challenge. Herein, we report an efficient annulation cascade reaction between cyclosulfonium salts and alkenes sulfur‐containing N ‐heterocycles by visible light/copper catalysis under mild conditions. The C—S bond cleavage/radical delivers variety corresponding containing aryl thioether motifs with good functional group tolerance. Significantly, current system could be used late‐stage functionalization complex bioactive molecules.

Язык: Английский

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Aerobic Oxidative Hydroxylation of Arylboronic Acids under Visible-Light Irradiation without Metal Catalysts or Additives

Organic Letters, Год журнала: 2024, Номер 26(9), С. 1959 - 1964

Опубликована: Фев. 26, 2024

Phenols are versatile synthetic intermediates and key structural motifs in many natural products biologically active compounds. We herein report a visible-light-induced aerobic oxidative hydroxylation of arylboronic acids/pinacol esters using air as oxidant without any catalysts base, etc., additives, providing green entry to variety phenols highly efficient concise fashion. This novel reaction is enabled by photoactivation an electron donor-acceptor complex, which THF serves both the solvent donor. DFT studies indicated that oxidation process involves concerted hydrogen abstraction transfer from dehydroxylation boronic acid undergoing spin crossover triplet singlet produce peroxoboronic intermidiate. Salient merits this chemistry include broad substrate scope excellent functional group tolerance, gram-scale synthesis, late-stage functionalizations well use air, visible light, catalyst- additive-free conditions. strategy introduces photoreaction mode with aid solvent, offering succinct environmentally sustainable route for synthesizing phenols. The strong practicability access modifying complex biorelevant molecules bode potential applications pharmaceutical chemistry.

Язык: Английский

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