Chemistry and biology of multicomponent reactions

A Domling, W Wang, K Wang - Chemical reviews, 2012 - ACS Publications
Multicomponent reactions (MCRs) are one-pot reactions employing more than two starting
materials, for example, 3, 4,..., 7, where most of the atoms of the starting materials are …

Drugging the p53 pathway: understanding the route to clinical efficacy

KH Khoo, CS Verma, DP Lane - Nature reviews Drug discovery, 2014 - nature.com
The tumour suppressor p53 is the most frequently mutated gene in human cancer, with more
than half of all human tumours carrying mutations in this particular gene. Intense efforts to …

Small-molecule inhibitors of the MDM2–p53 protein–protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment: miniperspective

Y Zhao, A Aguilar, D Bernard… - Journal of medicinal …, 2015 - ACS Publications
Design of small-molecule inhibitors (MDM2 inhibitors) to block the MDM2–p53 protein–
protein interaction has been pursued as a new cancer therapeutic strategy. In recent years …

Modulators of protein–protein interactions

LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014 - ACS Publications
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …

Recent applications of multicomponent reactions in medicinal chemistry

P Slobbe, E Ruijter, RVA Orru - MedChemComm, 2012 - pubs.rsc.org
Multicomponent reactions are flexible reactions for the rapid generation of complex
molecules with often biologically relevant scaffold structures. Combined with the ease of …

Multicomponent reactions, union of MCRs and beyond

T Zarganes‐Tzitzikas, AL Chandgude… - The Chemical …, 2015 - Wiley Online Library
Multicomponent reactions (MCRs), which are located between one‐and two‐component
and polymerization reactions, provide a number of valuable conceptual and synthetic …

A potent small-molecule inhibitor of the MDM2–p53 interaction (MI-888) achieved complete and durable tumor regression in mice

Y Zhao, S Yu, W Sun, L Liu, J Lu… - Journal of medicinal …, 2013 - ACS Publications
We previously reported the discovery of a class of spirooxindoles as potent and selective
small-molecule inhibitors of the MDM2–p53 interaction (MDM2 inhibitors). We report herein …

Progress and perspectives on directing group-assisted palladium-catalysed C–H functionalisation of amino acids and peptides

S Shabani, Y Wu, HG Ryan, CA Hutton - Chemical Society Reviews, 2021 - pubs.rsc.org
Peptide modifications can unlock a variety of compounds with structural diversity and
abundant biological activity. In nature, peptide modifications, such as functionalisation at the …

Multicomponent reactions as a potent tool for the synthesis of benzodiazepines

H Farhid, V Khodkari, MT Nazeri… - Organic & …, 2021 - pubs.rsc.org
Benzodiazepines (BZDs), a diverse class of benzofused seven-membered N-heterocycles,
display essential pharmacological properties and play vital roles in some biochemical …

State-of-the-art strategies for targeting protein–protein interactions by small-molecule inhibitors

C Sheng, G Dong, Z Miao, W Zhang… - Chemical Society …, 2015 - pubs.rsc.org
Targeting protein–protein interactions (PPIs) has emerged as a viable approach in modern
drug discovery. However, the identification of small molecules enabling us to effectively …