[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 …

Inhibition of RNA-binding proteins with small molecules

P Wu - Nature Reviews Chemistry, 2020 - nature.com
Protein–RNA interactions have crucial roles in various cellular activities, which, when
dysregulated, can lead to a range of human diseases. The identification of small molecules …

A high-throughput platform to identify small-molecule inhibitors of CRISPR-Cas9

B Maji, SA Gangopadhyay, M Lee, M Shi, P Wu… - Cell, 2019 - cell.com
The precise control of CRISPR-Cas9 activity is required for a number of genome
engineering technologies. Here, we report a generalizable platform that provided the first …

The Asymmetric Hetero‐Diels–Alder Reaction in the Syntheses of Biologically Relevant Compounds

V Eschenbrenner‐Lux, K Kumar… - Angewandte Chemie …, 2014 - Wiley Online Library
Abstract The hetero‐Diels–Alder reaction is one of the most powerful transformations in the
chemistry toolbox for the synthesis of aza‐and oxa‐heterocycles embodying multiple …

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 …

Catalytic Asymmetric Aza‐Diels‐Alder Reaction: Pivotal Milestones and Recent Applications to Synthesis of Nitrogen‐Containing Heterocycles

MG Vinogradov, OV Turova… - Advanced Synthesis & …, 2021 - Wiley Online Library
In this review, the pivotal achievements and recent advances in catalytic asymmetric aza‐
DAR reported up to 2020 are retrospectively considered and their potency for …

Catalytic asymmetric aza-Diels–Alder reactions: The Povarov cycloaddition reaction

M Fochi, L Caruana, L Bernardi - Synthesis, 2014 - thieme-connect.com
The Povarov reaction provides a straightforward and modular entry to 1, 2, 3, 4-
tetrahydroquinolines (THQs). Despite its importance, it was only very recently that several …

α-Imino esters in organic synthesis: recent advances

B Eftekhari-Sis, M Zirak - Chemical Reviews, 2017 - ACS Publications
α-Imino esters are useful precursors for the synthesis of a variety of types of natural and
unnatural α-amino acid derivatives, with a wide range of biological activities. Due to the …

Enantioselective Copper‐Catalyzed Quinoline Alkynylation

M Pappoppula, FSP Cardoso, BO Garrett… - Angewandte …, 2015 - Wiley Online Library
A highly enantioselective copper‐catalyzed alkynylation of quinolinium salts is reported. The
reaction employs StackPhos, a newly developed imidazole‐based chiral biaryl P, N ligand …

Micellar Brønsted acid mediated synthesis of DNA-tagged heterocycles

MK Škopić, K Gotte, C Gramse, M Dieter… - Journal of the …, 2019 - ACS Publications
The translation of well-established molecular biology methods such as genetic coding,
selection, and DNA sequencing to combinatorial organic chemistry and compound …