A Bridging Strategy for On‐DNA Dithiocarbamate Library Synthesis

Chemistry - An Asian Journal 2026

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Authors: Yagong Wang, Huanqing Zhang, Fanming Zeng, Xue Zhao, Junyun Chen, Lijun Xue, Kexin Yang, Yun Jin Hu
DOI: 10.1002/asia.70611
Cited by: 3
References: 25

Abstract

ABSTRACT Dithiocarbamates (DTCs) are privileged scaffolds in medicinal chemistry, yet inaccessible via DNA‐encoded libraries (DELs) due to a lack of robust on‐DNA synthesis. We developed a general procedure for on‐DNA DTC formation using a carbon disulfide (CS 2 ) bridging strategy. This method efficiently links diverse aliphatic secondary amines and alkyl halides under mild conditions with high conversions and excellent DNA compatibility. The utility of this method was demonstrated by constructing a prototype DEL, thereby bridging a critical gap in chemical space and facilitating the rapid discovery of DTC‐based therapeutics.

Fields of Study & Subjects

Chemical Synthesis and Analysis Click Chemistry and Applications Sulfur-Based Synthesis Techniques

Publication details

Journal / source
Chemistry - An Asian Journal
Publisher
Wiley
Volume
21
Issue
3
Pages
e70611–e70611
Publication date
31 January 2026
Language
EN