Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology

M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Advances in covalent kinase inhibitors

A Abdeldayem, YS Raouf, SN Constantinescu… - Chemical Society …, 2020 - pubs.rsc.org
Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Targeting pyruvate dehydrogenase kinase signaling in the development of effective cancer therapy

S Anwar, A Shamsi, T Mohammad, A Islam… - … et Biophysica Acta (BBA …, 2021 - Elsevier
Pyruvate is irreversibly decarboxylated to acetyl coenzyme A by mitochondrial pyruvate
dehydrogenase complex (PDC). Decarboxylation of pyruvate is considered a crucial step in …

Pyruvate dehydrogenase kinases (PDKs): an overview toward clinical applications

X Wang, X Shen, Y Yan, H Li - Bioscience Reports, 2021 - portlandpress.com
Pyruvate dehydrogenase kinase (PDK) can regulate the catalytic activity of pyruvate
decarboxylation oxidation via the mitochondrial pyruvate dehydrogenase complex, and it …

Metabolic flexibility in cancer: targeting the pyruvate dehydrogenase kinase: pyruvate dehydrogenase axis

BL Woolbright, G Rajendran, RA Harris… - Molecular cancer …, 2019 - AACR
Cancer cells use alterations of normal metabolic processes to sustain proliferation
indefinitely. Transcriptional and posttranscriptional control of the pyruvate dehydrogenase …

Overview of recent strategic advances in medicinal chemistry

G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
Introducing novel strategies, concepts, and technologies that speed up drug discovery and
the drug development cycle is of great importance both in the highly competitive …

Polysulfurating reagent design for unsymmetrical polysulfide construction

X Xiao, J Xue, X Jiang - Nature communications, 2018 - nature.com
From life science to material science, to pharmaceutical industry, and to food chemistry,
polysulfides are vital structural scaffolds. However, there are limited synthetic methods for …

Preparation of thiazole-2-thiones through TBPB-promoted oxidative cascade cyclization of enaminones with elemental sulfur

B Zhang, D Liu, Y Sun, Y Zhang, J Feng, F Yu - Organic Letters, 2021 - ACS Publications
An unprecedented method for the construction of thiazole-2-thiones via an oxidative
cascade cyclization strategy is described. The novel protocol involves the simultaneous …

Revealing quinquennial anticancer journey of morpholine: A SAR based review

F Arshad, MF Khan, W Akhtar, MM Alam… - European journal of …, 2019 - Elsevier
Morpholine, a six-membered heterocycle containing one nitrogen and one oxygen atom, is a
moiety of great significance. It forms an important intermediate in many industrial and …

An insight into medicinal attributes of dithiocarbamates: Bird's eye view

SD Shinde, AP Sakla, N Shankaraiah - Bioorganic Chemistry, 2020 - Elsevier
Dithiocarbamates are considered as an important motif owing to its extensive biological
applications in medicinal chemistry. The synthesis of this framework can easily be achieved …