Tetrazoles via multicomponent reactions

CG Neochoritis, T Zhao, A Domling - Chemical reviews, 2019 - ACS Publications
Tetrazole derivatives are a prime class of heterocycles, very important to medicinal
chemistry and drug design due to not only their bioisosterism to carboxylic acid and amide …

The Groebke‐Blackburn‐Bienaymé Reaction

A Boltjes, A Dömling - European Journal of Organic Chemistry, 2019 - Wiley Online Library
Imidazo [1, 2‐a] pyridine is a well‐known scaffold in many marketed drugs, such as
Zolpidem, Minodronic acid, Miroprofen and DS‐1 and it also serves as a broadly applied …

[HTML][HTML] Expansion of chemical space for collaborative lead generation and drug discovery: the European Lead Factory Perspective

A Karawajczyk, F Giordanetto, J Benningshof… - Drug Discovery …, 2015 - Elsevier
Highlights•High-quality compound collections are a main determinant of drug discovery
success.•Generation of relevant collections is a significant challenge for any …

Ugi Four-Component Reactions Using Alternative Reactants

SE Hooshmand, W Zhang - Molecules, 2023 - mdpi.com
The Ugi four-component reaction (Ugi-4CR) undoubtedly is the most prominent
multicomponent reaction (MCRs) that has sparked organic chemists' interest in the field. It …

Automated, accelerated nanoscale synthesis of iminopyrrolidines

A Osipyan, S Shaabani, R Warmerdam… - Angewandte …, 2020 - Wiley Online Library
Miniaturization and acceleration of synthetic chemistry is an emerging area in
pharmaceutical, agrochemical, and materials research and development. Herein, we …

Rapid approach to complex boronic acids

CG Neochoritis, S Shaabani… - Science …, 2019 - science.org
The compatibility of free boronic acid building blocks in multicomponent reactions to readily
create large libraries of diverse and complex small molecules was investigated …

[HTML][HTML] Novel SK channel positive modulators prevent ferroptosis and excitotoxicity in neuronal cells

Y Zhang, S Shaabani, K Vowinkel… - Biomedicine & …, 2024 - Elsevier
Small conductance calcium-activated potassium (SK) channel activity has been proposed to
play a role in the pathology of several neurological diseases. Besides regulating plasma …

Multicomponent reaction–derived covalent inhibitor space

F Sutanto, S Shaabani, CG Neochoritis… - Science …, 2021 - science.org
The area of covalent inhibitors is gaining momentum due to recently introduced clinical
drugs, but libraries of these compounds are scarce. Multicomponent reaction (MCR) …

Artificial macrocycles as potent p53–MDM2 inhibitors

N Estrada-Ortiz, CG Neochoritis… - ACS medicinal …, 2017 - ACS Publications
Based on a combination of an Ugi four component reaction and a ring closing metathesis, a
library of novel artificial macrocyclic inhibitors of the p53–MDM2 interaction was designed …

Selective steroidogenic cytochrome P450 haem iron ligation by steroid-derived isonitriles

AM Richard, NR Wong, K Harris, R Sundar… - Communications …, 2023 - nature.com
Alkyl isonitriles, R—NC, have previously been shown to ligate the heme (haem) iron of
cytochromes P450 in both accessible oxidation states (ferrous, Fe2+, and ferric, Fe3+) …