Journal
BIOCONJUGATE CHEMISTRY
Volume 29, Issue 11, Pages 3841-3846Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.8b00676
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Funding
- Welch Foundation [H-Q:0042]
- Cancer Prevention Research Institute of Texas (CPRIT) [RP160805]
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DNA-encoded chemical libraries (DELs) are a cost-effective technology for the discovery of novel chemical probes and drug candidates. A major limiting factor in assembling productive DELs is the availability of DNA-compatible chemical reactions in aqueous media. In an effort to increase the chemical accessibility and structural diversity of small molecules displayed by DELs, we developed a robust Suzuki-Miyaura reaction protocol that is compatible with the DNA structures. By employing a water-soluble Pd-precatalyst, we developed conditions that allow efficient coupling of DNA-linked aryl halides with a wide variety of boronic acids/esters including heteroaryl boronates.
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