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High-Density DNA and RNA microarrays - Photolithographic Synthesis, Hybridization and Preparation of Large Nucleic Acid Libraries

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Mask and Release Strategy-Enabled Diversity-Oriented Synthesis for DNA-Encoded Library.

Silin Zhang¹, Haiman Zhang¹, Xiawen Liu¹

¹Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target & Clinical Pharmacology, The NMPA and State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences and the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou, 511436, China.

Advanced Science (Weinheim, Baden-Wurttemberg, Germany)

|December 3, 2023

Summary

This study introduces a "Mask & Release" strategy for efficient on-DNA synthesis of diverse DNA-encoded library (DEL) core skeletons. This approach enhances chemical space coverage for drug discovery by enabling versatile C-H functionalization.

Keywords:

DNA-encoded library benzofuran diversity-oriented synthesis mask and release sulfiliminyl phenol

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Area of Science:

Synthetic Chemistry
Medicinal Chemistry
Molecular Biology

Background:

DNA-encoded libraries (DELs) are powerful tools for drug discovery.
Limited diversity in DELs is often due to challenges in synthesizing diverse on-DNA core skeletons.
Efficient methods for on-DNA synthesis are crucial for expanding DEL capabilities.

Purpose of the Study:

To develop a novel strategy for streamlined on-DNA synthesis of diverse DEL core skeletons.
To introduce a versatile method for creating complex, drug-like molecules directly on DNA.
To overcome limitations in current on-DNA synthetic approaches for DEL generation.

Main Methods:

A "Mask & Release" strategy utilizing N-phenoxyacetamide as a masked phenol and directing group.
DNA-compatible C-H functionalization to introduce the first dimension of diversity.
Subsequent release of phenol functionality for introducing the second dimension of diversity.

Main Results:

Demonstrated efficient on-DNA synthesis of various drug-like core skeletons, including ortho-alkenyl/sulfiliminyl/cyclopropyl phenol, benzofuran, and dihydrobenzofuran.
Successfully introduced two dimensions of diversity at defined sites on DNA.
Established a versatile platform for on-DNA core skeleton synthesis.

Conclusions:

The "Mask & Release" strategy significantly enhances the diversity of DNA-encoded libraries.
This method provides a paradigm for developing new on-DNA synthetic methodologies.
The approach facilitates the creation of novel chemical entities for drug discovery.