Issue 11, 2024

Modular synthesis of functional libraries by accelerated SuFEx click chemistry

Abstract

Accelerated SuFEx Click Chemistry (ASCC) is a powerful method for coupling aryl and alkyl alcohols with SuFEx-compatible functional groups. With its hallmark favorable kinetics and exceptional product yields, ASCC streamlines the synthetic workflow, simplifies the purification process, and is ideally suited for discovering functional molecules. We showcase the versatility and practicality of the ASCC reaction as a tool for the late-stage derivatization of bioactive molecules and in the array synthesis of sulfonate-linked, high-potency, microtubule targeting agents (MTAs) that exhibit nanomolar anticancer activity against multidrug-resistant cancer cell lines. These findings underscore ASCC's promise as a robust platform for drug discovery.

Graphical abstract: Modular synthesis of functional libraries by accelerated SuFEx click chemistry

Supplementary files

Article information

Article type
Edge Article
Submitted
26 окт 2023
Accepted
09 фев 2024
First published
04 мар 2024
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2024,15, 3879-3892

Modular synthesis of functional libraries by accelerated SuFEx click chemistry

J. A. Homer, R. A. Koelln, A. S. Barrow, T. L. Gialelis, Z. Boiarska, N. S. Steinohrt, E. F. Lee, W. Yang, R. M. Johnson, T. Chung, A. N. Habowski, D. S. Vishwakarma, D. Bhunia, C. Avanzi, A. D. Moorhouse, M. Jackson, D. A. Tuveson, S. K. Lyons, M. J. Lukey, W. D. Fairlie, S. M. Haider, M. O. Steinmetz, A. E. Prota and J. E. Moses, Chem. Sci., 2024, 15, 3879 DOI: 10.1039/D3SC05729A

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