Stephen C. Pelly
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View article: Identification and Characterization of Novel Chikungunya Virus Polymerase Inhibitors
Identification and Characterization of Novel Chikungunya Virus Polymerase Inhibitors Open
Chikungunya virus (CHIKV) and other alphaviruses in the Togaviridae family are positive-sense RNA viruses and major human pathogens, causing millions of infections worldwide. In humans, alphaviruses such as CHIKV, Mayaro and Ross River vir…
View article: Improved Rigidin-Inspired Antiproliferative Agents with Modifications on the 7-Deazahypoxanthine C7/C8 Ring Systems
Improved Rigidin-Inspired Antiproliferative Agents with Modifications on the 7-Deazahypoxanthine C7/C8 Ring Systems Open
To improve their aqueous solubility characteristics, water-solubilizing groups were added to some antiproliferative, rigidin-inspired 7-deazahypoxanthine frameworks after molecular modeling seemed to indicate that structural modifications …
View article: Design and Optimization of Novel Competitive, Non-peptidic, SARS-CoV-2 M<sup>pro</sup> Inhibitors
Design and Optimization of Novel Competitive, Non-peptidic, SARS-CoV-2 M<sup>pro</sup> Inhibitors Open
The SARS-CoV-2 main protease (Mpro) has been proven to be a highly effective target for therapeutic intervention, yet only one drug currently holds FDA approval status for this target. We were inspired by a series of publication…
View article: Discovery of 5′-Substituted 5-Fluoro-2′-deoxyuridine Monophosphate Analogs: A Novel Class of Thymidylate Synthase Inhibitors
Discovery of 5′-Substituted 5-Fluoro-2′-deoxyuridine Monophosphate Analogs: A Novel Class of Thymidylate Synthase Inhibitors Open
5-Fluorouracil and 5-fluorouracil-based prodrugs have been used clinically for decades to treat cancer. Their anticancer effects are most prominently ascribed to inhibition of thymidylate synthase (TS) by metabolite 5-fluoro-2'-deoxyuridin…
View article: Covalent Allosteric Inhibitors of Akt Generated Using a Click Fragment Approach
Covalent Allosteric Inhibitors of Akt Generated Using a Click Fragment Approach Open
Akt is a protein kinase that has been implicated in the progression of cancerous tumours. A number of covalent allosteric Akt inhibitors are known, and based on these scaffolds, a small library of novel potential covalent allosteric imidaz…
View article: CCDC 2083857: Experimental Crystal Structure Determination
CCDC 2083857: Experimental Crystal Structure Determination Open
View article: The Negative Allosteric Modulator EU1794-4 Reduces Single-Channel Conductance and Ca2+ Permeability of GluN1/GluN2A N-Methyl-d-Aspartate Receptors
The Negative Allosteric Modulator EU1794-4 Reduces Single-Channel Conductance and Ca2+ Permeability of GluN1/GluN2A N-Methyl-d-Aspartate Receptors Open
View article: Potent SARS-CoV-2 Direct-Acting Antivirals Provide an Important Complement to COVID-19 Vaccines
Potent SARS-CoV-2 Direct-Acting Antivirals Provide an Important Complement to COVID-19 Vaccines Open
View article: [3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor
[3 + 2]-Annulation of pyridinium ylides with 1-chloro-2-nitrostyrenes unveils a tubulin polymerization inhibitor Open
Heterocycles prepared via [3 + 2]-cycloaddition of pyridinium ylides to 1-chloro-2-nitrostyrenes were evaluated as microtubule-targeting anticancer agents potent against BE(2)-C neuroblastoma cells.
View article: Synthesis of pyrrolocarbazoles with N-substituted alkynyl-, alkylcyano- and alkylhydroxyl-groups
Synthesis of pyrrolocarbazoles with N-substituted alkynyl-, alkylcyano- and alkylhydroxyl-groups Open
CITATION: Van der Westhuyzen, A. E. et al. 2020. Synthesis of pyrrolocarbazoles with N-substituted alkynyl-, alkylcyano- and alkylhydroxyl-groups. Arkivoc, v:129-147, doi:10.24820/ark.5550190.p011.412.
View article: CCDC 2002775: Experimental Crystal Structure Determination
CCDC 2002775: Experimental Crystal Structure Determination Open
View article: CCDC 2002762: Experimental Crystal Structure Determination
CCDC 2002762: Experimental Crystal Structure Determination Open
View article: Accelerated Discovery of Potent Fusion Inhibitors for Respiratory Syncytial Virus
Accelerated Discovery of Potent Fusion Inhibitors for Respiratory Syncytial Virus Open
A series of five benzimidazole-based compounds were identified using a machine learning algorithm as potential inhibitors of the respiratory syncytial virus (RSV) fusion protein. These compounds were synthesized, and compound 2 in p…
View article: Synthesis of 2-substituted tetrahydroisoquinolin-6-ols: potential scaffolds for estrogen receptor modulation and/or microtubule degradation
Synthesis of 2-substituted tetrahydroisoquinolin-6-ols: potential scaffolds for estrogen receptor modulation and/or microtubule degradation Open
CITATION: Mabank, T., et al. 2019. Synthesis of 2-substituted tetrahydroisoquinolin-6-ols: potential scaffolds for estrogen receptor modulation and / or microtubule degradation. ARKIVOC, iv:245-279, doi:10.24820/ark.5550190.p010.962.
View article: Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors Open
Since the discovery of HIV as the etiological agent of AIDS, the virus has infected millions of people each year. Fortunately, with the use of HAART, viremia can be suppressed to below detectable levels in the infected individuals, which s…
View article: The Amaryllidaceae Alkaloid Haemanthamine Binds the Eukaryotic Ribosome to Repress Cancer Cell Growth
The Amaryllidaceae Alkaloid Haemanthamine Binds the Eukaryotic Ribosome to Repress Cancer Cell Growth Open
View article: CCDC 1504092: Experimental Crystal Structure Determination
CCDC 1504092: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1504091: Experimental Crystal Structure Determination
CCDC 1504091: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities
Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities Open
Docking studies of tubulin-targeting C2-substituted 7-deazahypoxanthine analogues of marine alkaloid rigidins led to the design and synthesis of compounds containing linear C2-substituents. The C2-alkynyl analogue was found to have double-…
View article: Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9‐Epipolygodial against Drug‐Resistant Cancer Cells
Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9‐Epipolygodial against Drug‐Resistant Cancer Cells Open
Polygodial, a terpenoid dialdehyde isolated from Polygonum hydropiper L., is a known agonist of the transient receptor potential vanilloid 1 (TRPV1). In this investigation a series of polygodial analogues were prepared and investigated for…
View article: Wittig derivatization of sesquiterpenoid polygodial leads to cytostatic agents with activity against drug resistant cancer cells and capable of pyrrolylation of primary amines
Wittig derivatization of sesquiterpenoid polygodial leads to cytostatic agents with activity against drug resistant cancer cells and capable of pyrrolylation of primary amines Open