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 Oct 2023
Accepted
09 Feb 2024
First published
04 Mar 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

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. You can use material from this article in other publications, without requesting further permission from the RSC, provided that the correct acknowledgement is given and it is not used for commercial purposes.

To request permission to reproduce material from this article in a commercial publication, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party commercial publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements