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Updated: Feb 2, 2026

High-Density DNA and RNA microarrays - Photolithographic Synthesis, Hybridization and Preparation of Large Nucleic Acid Libraries
Published on: August 12, 2019
A Bridging Strategy for On-DNA Dithiocarbamate Library Synthesis
Yagong Wang1, Huanqing Zhang1, Fanming Zeng1
1Pharmaron (Ningbo) Technology Development Co., Ltd., Ningbo, China.
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 (CS2) 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.
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