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Modular synthesis of functional libraries by accelerated SuFEx click chemistry

Homer, JA; Koelln, RA; Barrow, AS; Gialelis, TL; Boiarska, Z; Steinohrt, NS; Lee, EF; ... Moses, JE; + view all (2024) Modular synthesis of functional libraries by accelerated SuFEx click chemistry. Chemical Science , 15 (11) pp. 3879-3892. 10.1039/d3sc05729a. Green open access

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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.

Type: Article
Title: Modular synthesis of functional libraries by accelerated SuFEx click chemistry
Location: England
Open access status: An open access version is available from UCL Discovery
DOI: 10.1039/d3sc05729a
Publisher version: https://doi.org/10.1039/D3SC05729A
Language: English
Additional information: This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/10189614
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