Modular synthesis of functional libraries by accelerated SuFEx click chemistry

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:	Homer, Joshua Koelln, Rebecca Yang, Wen-Hsuan Tuveson, David A. Lyons, Scott Lukey, Michael Moses, John E. Chung, Taemoon Habowski, Amber N. Moorhouse, Adam Johnson, Robert Vishwakarma, Dharmendra Bhunia, Debmalya
Communities:	CSHL labs > Lyons lab CSHL labs > Tuveson lab CSHL labs > Wigler lab CSHL labs > Lukey lab CSHL labs > Moses lab CSHL Cancer Center Program CSHL Cancer Center Program > Cellular Communication in Cancer Program CSHL Cancer Center Program > Gene Regulation and Inheritance Program CSHL Cancer Center Shared Resources > Mass Spectrometry Service CSHL Cancer Center Shared Resources > Organoid Service
SWORD Depositor:	CSHL Elements
Depositing User:	CSHL Elements
Date:	13 March 2024
Date Deposited:	18 Mar 2024 13:12
Last Modified:	18 Mar 2024 13:12
PMCID:	PMC10935723
Related URLs:	Publisher
Dataset ID:	https://www.rcsb.org/ PDB 8RIV
URI:	https://repository.cshl.edu/id/eprint/41466

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