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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.

SUBMITTER: Homer JA

PROVIDER: S-EPMC10935723 | biostudies-literature | 2024 Mar

REPOSITORIES: biostudies-literature

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Modular synthesis of functional libraries by accelerated SuFEx click chemistry.

Homer Joshua A JA Koelln Rebecca A RA Barrow Andrew S AS Gialelis Timothy L TL Boiarska Zlata Z Steinohrt Nikita S NS Lee Erinna F EF Yang Wen-Hsuan WH Johnson Robert M RM Chung Taemoon T Habowski Amber N AN Vishwakarma Dharmendra S DS Bhunia Debmalya D Avanzi Charlotte C Moorhouse Adam D AD Jackson Mary M Tuveson David A DA Lyons Scott K SK Lukey Michael J MJ Fairlie W Douglas WD Haider Shozeb M SM Steinmetz Michel O MO Prota Andrea E AE Moses John E JE

Chemical science 20240304 11

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 syn ...[more]

PMID: 38487227

Dataset Information

Modular synthesis of functional libraries by accelerated SuFEx click chemistry.

Publications

Modular synthesis of functional libraries by accelerated SuFEx click chemistry.

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