Modular synthesis of functional libraries by accelerated SuFEx click chemistry

Author:

Homer Joshua A.1ORCID,Koelln Rebecca A.1ORCID,Barrow Andrew S.2ORCID,Gialelis Timothy L.2ORCID,Boiarska Zlata34ORCID,Steinohrt Nikita S.56ORCID,Lee Erinna F.567ORCID,Yang Wen-Hsuan1ORCID,Johnson Robert M.1ORCID,Chung Taemoon1ORCID,Habowski Amber N.1ORCID,Vishwakarma Dharmendra S.1ORCID,Bhunia Debmalya1ORCID,Avanzi Charlotte8ORCID,Moorhouse Adam D.1,Jackson Mary8ORCID,Tuveson David A.1ORCID,Lyons Scott K.1ORCID,Lukey Michael J.1ORCID,Fairlie W. Douglas567ORCID,Haider Shozeb M.9ORCID,Steinmetz Michel O.310ORCID,Prota Andrea E.3ORCID,Moses John E.1ORCID

Affiliation:

1. Cancer Center, Cold Spring Harbor Laboratory, 1 Bungtown Rd, Cold Spring Harbor, NY 11724, USA

2. La Trobe Institute for Molecular Science, La Trobe University, Melbourne, VIC 3086, Australia

3. Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut, Villigen PSI, 5232, Switzerland

4. Department of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133 Milan, Italy

5. Olivia Newton-John Cancer Research Institute, Heidelberg, Victoria, 3084, Australia

6. School of Cancer Medicine, La Trobe University, Melbourne, Victoria, 3086, Australia

7. Department of Biochemistry and Chemistry, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria, 3086, Australia

8. Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, CO 80523, USA

9. School of Pharmacy, University College London, 29-39 Brunswick Square, London, WC1N 1AX, UK

10. Biozentrum, University of Basel, 4056 Basel, Switzerland

Abstract

The Accelerated SuFEx Click Chemistry (ASCC) protocol, adapted to a 96-well plate format, has been applied to the late-stage derivatization of bioactive molecules and array synthesis of anticancer agents, showcasing its potential for drug discovery.

Funder

National Cancer Institute

La Trobe University

New York Community Trust

American Cancer Society

F. M. Kirby Foundation

METAvivor

Australian Research Council

Lustgarten Foundation

Victorian Cancer Agency

Cold Spring Harbor Laboratory

Northwell Health

Starr Foundation

Swim Across America

U.S. Department of Defense

Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung

University of Minnesota

Publisher

Royal Society of Chemistry (RSC)

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