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[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology
CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …
probes of disease-related targets and potential starting points for drug discovery. In this …
Targeting the pancreatic β-cell to treat diabetes
A Vetere, A Choudhary, SM Burns… - Nature reviews Drug …, 2014 - nature.com
Diabetes is a leading cause of morbidity and mortality worldwide, and predicted to affect
over 500 million people by 2030. However, this growing burden of disease has not been met …
over 500 million people by 2030. However, this growing burden of disease has not been met …
Scaffold diversity synthesis and its application in probe and drug discovery
M Garcia‐Castro, S Zimmermann… - Angewandte Chemie …, 2016 - Wiley Online Library
Scaffold diversity is a crucial feature of compound collections that has a huge impact on their
success in biological screenings. The synthesis of highly complex and diverse scaffolds …
success in biological screenings. The synthesis of highly complex and diverse scaffolds …
Recent achievements and current trajectories of diversity-oriented synthesis
CJ Gerry, SL Schreiber - Current Opinion in Chemical Biology, 2020 - Elsevier
For two decades, diversity-oriented synthesis (DOS) has facilitated the assembly of small-
molecule libraries comprising a variety of complex molecular architectures. Here, we …
molecule libraries comprising a variety of complex molecular architectures. Here, we …
[HTML][HTML] Synthesis of medium-sized heterocycles by transition-metal-catalyzed intramolecular cyclization
Medium-sized heterocycles (with 8 to 11 atoms) constitute important structural components
of several biologically active natural compounds and represent promising scaffolds in …
of several biologically active natural compounds and represent promising scaffolds in …
[HTML][HTML] Emerging diabetes therapies: Bringing back the β-cells
Background Stem cell therapies are finally coming of age as a viable alternative to
pancreatic islet transplantation for the treatment of insulin-dependent diabetes. Several …
pancreatic islet transplantation for the treatment of insulin-dependent diabetes. Several …
Recent applications of diversity-oriented synthesis toward novel, 3-dimensional fragment collections
SL Kidd, TJ Osberger, N Mateu, HF Sore… - Frontiers in …, 2018 - frontiersin.org
Fragment-based drug discovery (FBDD) is a well-established approach for the discovery of
novel medicines, illustrated by the approval of two FBBD-derived drugs. This methodology is …
novel medicines, illustrated by the approval of two FBBD-derived drugs. This methodology is …
[ΒΙΒΛΙΟ][B] Studies in natural products chemistry
A Rahman - 2023 - books.google.com
Studies in Natural Products Chemistry, Volume 79 covers the synthesis, testing and
recording of the medicinal properties of natural products, providing cutting-edge accounts of …
recording of the medicinal properties of natural products, providing cutting-edge accounts of …
[HTML][HTML] Recent strides in the transition metal-free cross-coupling of haloacetylenes with electron-rich heterocycles in solid media
LN Sobenina, BA Trofimov - Molecules, 2020 - mdpi.com
The publications covering new, transition metal-free cross-coupling reactions of pyrroles
with electrophilic haloacetylenes in solid medium of metal oxides and salts to …
with electrophilic haloacetylenes in solid medium of metal oxides and salts to …
Diversity-oriented synthesis encoded by deoxyoligonucleotides
L Hudson, JW Mason, MV Westphal… - nature …, 2023 - nature.com
Diversity-oriented synthesis (DOS) is a powerful strategy to prepare molecules with
underrepresented features in commercial screening collections, resulting in the elucidation …
underrepresented features in commercial screening collections, resulting in the elucidation …