University of Groningen
Target-based drug discovery: from protein structure to small-molecules by MCR chemistry
Wang, Yuanze
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Publication date: 2018
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Wang, Y. (2018). Target-based drug discovery: from protein structure to small-molecules by MCR chemistry. University of Groningen.
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Target-based Drug Discovery:
From Protein Structure to
Small-Molecules by
MCR Chemistry
Page | 2
PhD Thesis
Target-based Drug Discovery: From Protein Structure to Small-Molecules by
MCR Chemistry
The research presented in this thesis was performed in the research group of Drug
Design of Groningen Research Institute of Pharmacy at the University of
Groningen, the Netherlands. The author thanks the financial support from the
Chinese Scholarship Council (CSC).
ISBN: 978-94-034-0958-0 (PDF without DRM)
ISBN: 978-94-034-0959-7 (Printed book)
Layout: Yuanze Wang
Cover design: Yuanze Wang
Printed by: Ipskamp Printing
Copyright © Yuanze Wang, Groningen, 2018
All rights reserved. No part of this thesis may be reproduced in any form or by
any means without prior permission of the author.
Target-based Drug Discovery: From
Protein Structure to
Small-Molecules by MCR Chemistry
PhD thesis
to obtain the degree of PhD at the
University of Groningen
on the authority of the
Rector Magnificus Prof. E. Sterken
and in accordance with
the decision by the College of Deans.
This thesis will be defended in public on
Monday 10 September 2018 at 09.00 hours
by
Yuanze Wang
born on 5 April 1989
in Shandong, China
Page | 4
Supervisors
Prof. A.S.S. Dömling
Co-supervisors
Dr. M.R. Groves
Assessment Committee
Prof. P.H. Elsinga
Prof. A.J. Minnaard
Prof. L. Banfi
Contents
Chapter 1
General Introduction and Scope of this Thesis ... 7
Chapter 2 A Systematic Protein Refolding Screen Method using the DGR Approach Reveals that Time and Secondary TSA are Essential Variables ... 29
Chapter 3 Easy Synthesis of Two Positional Isomeric Tetrazole Libraries ... 55
Chapter 4 Two Cycles with One Catch: Hydrazine in Ugi 4-CR and its Post-cyclizations ... 83
Chapter 5 Efficient and Diverse Synthesis of Isoquinoline Derivatives and Benzo[d]azepinone Scaffolds by New Ugi/Pomeranz–Fritsch Reaction ... 119
Chapter 6 Acoustic Dispensing-Enabled Reaction Scouting ... 149
Summary ... 179
Samenvatting ... 181
Publication ... 183
