On-DNA Mannich Reaction for DNA-Encoded Library Synthesis DOI
Danila Ryzhikh, Hyewon Seo, Jihoon Lee

et al.

The Journal of Organic Chemistry, Journal Year: 2024, Volume and Issue: 89(22), P. 16957 - 16963

Published: Nov. 1, 2024

The β-amino ketones produced through the Mannich reaction hold significant potential as candidates for various drugs. In this study, we optimized on-DNA conditions and applied them to investigate reactions of DNA-conjugated aldehydes with amine ketone building blocks. developed preserved DNA integrity established viable routes library production. These results underscore in DNA-encoded (DEL) synthesis.

Language: Английский

On-DNA Medicinal Chemistry: Focused Libraries, Fragment Expansion, and Hit Optimisation DOI
Harriet A. Stanway‐Gordon, Michael J. Waring

Royal Society of Chemistry eBooks, Journal Year: 2025, Volume and Issue: unknown, P. 87 - 118

Published: Feb. 21, 2025

Since their inception thirty years ago, DNA-encoded libraries (DELs) have proven to be a formidable technique for naïve hit finding, with implementation facilitating the generation of lead-series across wide range target classes. In recent however, it has been demonstrated that utility DELs within drug discovery need not restricted this purpose, variety strategies being adopted broaden impact encoded field. Discussed herein are current applications wider medicinal chemistry pipeline, including application and focused libraries; use fragment expansion; potential facilitation optimisation processes. The state field is assessed, future directions technology area explored.

Language: Английский

Citations

0
Photoinduced Site-Selective Alkylation Enabling Synthesis of C-3-Alkylated Quinoxalinone on DNA DOI

Kyeong Seop Kim,

Junseok Ra,

Madala Hari Babu

et al.

Organic Letters, Journal Year: 2025, Volume and Issue: unknown

Published: April 30, 2025

A mild and biocompatible strategy for the site-selective alkylation of quinoxalinones via photoinduced dehydrogenative has been developed. This protocol enables functionalization both unprotected quinoxalinone nonreactive dihydroquinoxalinone under DNA-compatible conditions. The optimized reaction proceeds efficiently while tolerating a diverse range alkyl donors from various radical precursors. Given its simplicity DNA compatibility, this methodology offers platform construction DNA-encoded libraries incorporating privileged scaffold.

Language: Английский

Citations

0
On-DNA Mannich Reaction for DNA-Encoded Library Synthesis DOI
Danila Ryzhikh, Hyewon Seo, Jihoon Lee

et al.

The Journal of Organic Chemistry, Journal Year: 2024, Volume and Issue: 89(22), P. 16957 - 16963

Published: Nov. 1, 2024

The β-amino ketones produced through the Mannich reaction hold significant potential as candidates for various drugs. In this study, we optimized on-DNA conditions and applied them to investigate reactions of DNA-conjugated aldehydes with amine ketone building blocks. developed preserved DNA integrity established viable routes library production. These results underscore in DNA-encoded (DEL) synthesis.

Language: Английский

Citations

1