Progress in the Synthesis and Transformations of Alkylidenecyclopropanes and Alkylidenecyclobutanes

A Brandi, S Cicchi, FM Cordero, A Goti - Chemical Reviews, 2014 - ACS Publications
Methylene-and alkylidenecyclopropanes (MCPs and ACPs, 1, Figure 1) and-cyclobutanes
(MCBs and ACBs, 2, Figure 1) are highly strained molecules, but at the same time most of …

Glycogen synthase kinase-3: A potential target for diabetes

DM Teli, AK Gajjar - Bioorganic & medicinal chemistry, 2023 - Elsevier
Elevated circulating glucose level due to β-cell dysfunction has been a key marker of Type-II
diabetes. Glycogen synthase kinase-3 (GSK-3) has been recognized as an enzyme involved …

[HTML][HTML] Structural simplification: an efficient strategy in lead optimization

S Wang, G Dong, C Sheng - Acta Pharmaceutica Sinica B, 2019 - Elsevier
The trend toward designing large hydrophobic molecules for lead optimization is often
associated with poor drug-likeness and high attrition rates in drug discovery and …

CDC7 inhibition blocks pathological TDP‐43 phosphorylation and neurodegeneration

NF Liachko, PJ McMillan, CR Guthrie… - Annals of …, 2013 - Wiley Online Library
Objective Kinase hyperactivity occurs in both neurodegenerative disease and cancer.
Lesions containing hyperphosphorylated aggregated TDP‐43 characterize amyotrophic …

Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core

P Sivaprakasam, X Han, RL Civiello… - Bioorganic & medicinal …, 2015 - Elsevier
Abstract Glycogen synthase kinase-3 (GSK-3) has been proposed to play a crucial role in
the pathogenesis of many diseases including cancer, stroke, bipolar disorders, diabetes and …

Aminopyrimidines: Recent synthetic procedures and anticancer activities

E Venturini Filho, EMC Pinheiro, S Pinheiro, SJ Greco - Tetrahedron, 2021 - Elsevier
The pyrimidine scaffold represents one of the privileged structures in chemistry, and there
has been an increase in number of studies utilizing this scaffold and its derivatives. The …

Discovery of XL413, a potent and selective CDC7 inhibitor

ES Koltun, AL Tsuhako, DS Brown, N Aay… - Bioorganic & medicinal …, 2012 - Elsevier
CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and
maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell …

Starting DNA synthesis: Initiation processes during the replication of chromosomal DNA in humans

HP Nasheuer, AM Meaney - Genes, 2024 - mdpi.com
The initiation reactions of DNA synthesis are central processes during human chromosomal
DNA replication. They are separated into two main processes: the initiation events at …

Rhodium (III) Complex with a Bulky Cyclopentadienyl Ligand as a Catalyst for Regioselective Synthesis of Dihydroisoquinolones through C− H Activation of …

EA Trifonova, NM Ankudinov, MV Kozlov… - … A European Journal, 2018 - Wiley Online Library
Catalytic reaction of arylhydroxamic acids with alkenes represents a convenient method for
preparation of biologically active dihydroisoquinolones. Here, the rhodium (III) complex …

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding

M Menichincheri, C Albanese, C Alli… - Journal of medicinal …, 2010 - ACS Publications
Cdc7 serine/threonine kinase is a key regulator of DNA synthesis in eukaryotic organisms.
Cdc7 inhibition through si RNA or prototype small molecules causes p53 independent …