Dearomative intermolecular [2 + 2] photocycloaddition for construction of C(sp3)-rich heterospirocycles on-DNA DOI Creative Commons
Longbo Li, Bianca T. Matsuo,

Guillaume Levitre

и другие.

Chemical Science, Год журнала: 2023, Номер 14(10), С. 2713 - 2720

Опубликована: Янв. 1, 2023

Diverse DNA-encoded libraries of complex and novel sp 3 -rich spirocycles were achieved using a versatile operationally simple visible light-mediated intermolecular [2 + 2] cycloaddition.

Язык: Английский

Discovery Small-Molecule p300 Inhibitors Derived from a Newly Developed Indazolone-Focused DNA-Encoded Library DOI

Yanrui Suo,

Kaige Li, Xing Yi Ling

и другие.

Bioconjugate Chemistry, Год журнала: 2024, Номер 35(8), С. 1251 - 1257

Опубликована: Авг. 8, 2024

The DNA-encoded library (DEL) is a robust tool for chemical biology and drug discovery. In this study, we developed DNA-compatible light-promoted reaction that highly efficient plate-compatible DEL construction based on the formation of indazolone scaffold. Employing high-efficiency approach, constructed featuring an core, which enabled identification novel series ligands specifically targeting E1A-binding protein (p300) after selection. Taken together, our findings underscore feasibility reactions in synthesis unveil promising avenues developing p300-targeting inhibitors.

Язык: Английский

Процитировано

3
Synthesis of Thiohydantoin Scaffolds on DNA for Focused DNA-Encoded Library Construction DOI
Xianfu Fang,

Yunzhu Ju,

Jiayou Wang

и другие.

Organic Letters, Год журнала: 2024, Номер unknown

Опубликована: Окт. 3, 2024

Thiohydantoin represents a significant class of biologically active privileged heterocyclic scaffolds. Herein, we present convenient and robust DNA-compatible method for constructing thiohydantoin-focused DNA-encoded library. This reaction can be applied to wide variety isothiocyanate partners, arylamine feedstocks, diverse α-amine acid derivatives, exhibiting excellent conversions, high functional group tolerance, preservation DNA tag integrity. Our allows easy access valuable three-cycle

Язык: Английский

Процитировано

3
Visible-Light-Induced Synergistic W/Cr Catalyzed gem-Difluoroallylation of Unactivated Alkanes DOI
Zhijie Zhang, Yue Zhang,

Xinyu Xie

и другие.

Organic Letters, Год журнала: 2025, Номер unknown

Опубликована: Фев. 19, 2025

Currently, the scope of Nozaki-Hiyama-Kishi (NHK) reaction is limited to aldehydes and ketones construct alcohol derivatives. Herein, we have described a visible-light-induced synergistic W/Cr(III)-catalyzed NHK-type gem-difluoroallylation unactivated cyclic linear alkanes. The merits feedstock materials, mild conditions, wide functionality tolerance. Mechanistic studies imply favorable reduction CrCl3 CrCl2 by reduced decatungstate W10O325-, thus closing catalytic cycle.

Язык: Английский

Процитировано

0
Photochemical-Promoted Cross-Coupling Reaction of Alkyl Boronate Esters with DNA-Conjugated Aryl Bromides for DNA-Encoded Library Synthesis DOI

Baiyang Mu,

Yiwei Zhang, Xudong Wang

и другие.

Bioconjugate Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Март 27, 2025

The C(sp2)-C(sp3) cross-coupling reaction is an effective way to increase the C(sp3) content in compound collections for drug discovery, enhancing molecular diversity and offering a unique chemistry starting point. In this study, we report mild, DNA-compatible, off-DNA-inert photochemical inspired by amino radical transfer strategy. This method demonstrates broad substrate scopes DNA-encoded library (DEL) constructions, utilizing commonly available structures on DNA diverse alkyl boronate ester building blocks, which have not been widely applied current DEL chemical space.

Язык: Английский

Процитировано

0
Dearomative intermolecular [2 + 2] photocycloaddition for construction of C(sp3)-rich heterospirocycles on-DNA DOI Creative Commons
Longbo Li, Bianca T. Matsuo,

Guillaume Levitre

и другие.

Chemical Science, Год журнала: 2023, Номер 14(10), С. 2713 - 2720

Опубликована: Янв. 1, 2023

Diverse DNA-encoded libraries of complex and novel sp 3 -rich spirocycles were achieved using a versatile operationally simple visible light-mediated intermolecular [2 + 2] cycloaddition.

Язык: Английский

Процитировано

8