Homer, Joshua A, Koelln, Rebecca A, Barrow, Andrew S, Gialelis, Timothy L, Boiarska, Zlata, Steinohrt, Nikita S, Lee, Erinna F, Yang, Wen-Hsuan, Johnson, Robert M, Chung, Taemoon, Habowski, Amber N, Vishwakarma, Dharmendra S, Bhunia, Debmalya, Avanzi, Charlotte, Moorhouse, Adam D, Jackson, Mary, Tuveson, David A, Lyons, Scott K, Lukey, Michael J, Fairlie, W Douglas, Haider, Shozeb M, Steinmetz, Michel O, Prota, Andrea E, Moses, John E (March 2024) Modular synthesis of functional libraries by accelerated SuFEx click chemistry. Chemical Science, 15 (11). pp. 3879-3892. ISSN 2041-6520 (Public Dataset)
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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.
| Item Type: | Paper |
|---|---|
| Subjects: | chemistry > techniques > click chemistry > Accelerated SuFEx Click Chemistry chemistry chemistry > techniques > click chemistry chemistry > techniques |
| CSHL Authors: | |
| Communities: | CSHL Cancer Center Program CSHL Cancer Center Program > Cellular Communication in Cancer Program CSHL Cancer Center Shared Resources > Mass Spectrometry Service CSHL Cancer Center Shared Resources > Organoid Service CSHL labs > Lyons lab CSHL labs > Tuveson lab CSHL labs > Wigler lab CSHL labs > Lukey lab CSHL labs > Moses lab |
| SWORD Depositor: | CSHL Elements |
| Depositing User: | CSHL Elements |
| Date: | 13 March 2024 |
| Date Deposited: | 18 Mar 2024 13:12 |
| Last Modified: | 29 Apr 2024 18:13 |
| PMCID: | PMC10935723 |
| Related URLs: | |
| Dataset ID: |
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| URI: | https://repository.cshl.edu/id/eprint/41466 |
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