Recent advances on small-molecule bromodomain-containing histone acetyltransferase inhibitors
M Liu, K Zhang, Q Li, H Pang, Z Pan… - Journal of Medicinal …, 2023 - ACS Publications
In recent years, substantial research has been conducted on molecular mechanisms and
inhibitors targeting bromodomains (BRDs) and extra-terminal (BET) family proteins. On this …
inhibitors targeting bromodomains (BRDs) and extra-terminal (BET) family proteins. On this …
[HTML][HTML] Acetyl-CoA metabolism as a therapeutic target for cancer
G Chen, B Bao, Y Cheng, M Tian, J Song… - Biomedicine & …, 2023 - Elsevier
Acetyl-coenzyme A (acetyl-CoA), an essential metabolite, not only takes part in numerous
intracellular metabolic processes, powers the tricarboxylic acid cycle, serves as a key hub …
intracellular metabolic processes, powers the tricarboxylic acid cycle, serves as a key hub …
In vitro and computational investigations of novel synthetic carboxamide-linked pyridopyrrolopyrimidines with potent activity as SARS-CoV-2-M Pro inhibitors
An essential target for COVID-19 is the main protease of SARS-CoV-2 (Mpro). With the
objective of targeting this receptor, a novel set of pyrido [1, 2-a] pyrrolo [2, 3-d] pyrimidines …
objective of targeting this receptor, a novel set of pyrido [1, 2-a] pyrrolo [2, 3-d] pyrimidines …
Apoptosis induction, PARP-1 inhibition, and cell cycle analysis of leukemia cancer cells treated with novel synthetic 1, 2, 3-triazole-chalcone conjugates
Leukemia is a life-threatening nonepithelial malignant disorder that is characterized by
uncontrolled growth of the hematopoietic cells. To date, there are still unmet needs for …
uncontrolled growth of the hematopoietic cells. To date, there are still unmet needs for …
From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity
Inhibition of PCAF bromodomain has been validated as a promising strategy for the
treatment of cancer. In this study, we report the bioisosteric modification of the first reported …
treatment of cancer. In this study, we report the bioisosteric modification of the first reported …
The antimicrobial potential and pharmacokinetic profiles of novel quinoline-based scaffolds: synthesis and in silico mechanistic studies as dual DNA gyrase and …
MH El-Shershaby, KM El-Gamal, AH Bayoumi… - New Journal of …, 2021 - pubs.rsc.org
The resistance of pathogenic microbes to currently available antimicrobial agents has been
considered a global alarming concern. Hence, close attention should be paid to the …
considered a global alarming concern. Hence, close attention should be paid to the …
Phenylpyrazolone-1, 2, 3-triazole hybrids as potent antiviral agents with promising SARS-CoV-2 main protease inhibition potential
COVID-19 infection is now considered one of the leading causes of human death. As an
attempt towards the discovery of novel medications for the COVID-19 pandemic, nineteen …
attempt towards the discovery of novel medications for the COVID-19 pandemic, nineteen …
Pharmacophore‐linked pyrazolo[3,4‐d]pyrimidines as EGFR‐TK inhibitors: Synthesis, anticancer evaluation, pharmacokinetics, and in silico mechanistic studies
Targeting the epidermal growth factor receptors (EGFRs) with small inhibitor molecules has
been validated as a potential therapeutic strategy in cancer therapy. Pyrazolo [3, 4‐d] …
been validated as a potential therapeutic strategy in cancer therapy. Pyrazolo [3, 4‐d] …
The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico …
Abstract Treatment options for the management of breast cancer are still inadequate. This
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …
Phthalazine‐based VEGFR‐2 inhibitors: Rationale, design, synthesis, in silico, ADMET profile, docking, and anticancer evaluations
F Khedr, MK Ibrahim, IH Eissa… - Archiv der …, 2021 - Wiley Online Library
In the designed compounds, a new linker was inserted in the form of fragments with verified
VEGFR‐2 inhibitory potential, including an α, β‐unsaturated ketonic fragment, pyrazole, and …
VEGFR‐2 inhibitory potential, including an α, β‐unsaturated ketonic fragment, pyrazole, and …