[HTML][HTML] Structural manipulations of marine natural products inspire a new library of 3-amino-1, 2, 4-triazine PDK inhibitors endowed with antitumor activity in …

D Carbone, M De Franco, C Pecoraro, D Bassani… - Marine Drugs, 2023 - mdpi.com
Pancreatic ductal adenocarcinoma (PDAC) is one of the main aggressive types of cancer,
characterized by late prognosis and drug resistance. Among the main factors sustaining …

1, 2, 4-Amino-triazine derivatives as pyruvate dehydrogenase kinase inhibitors: Synthesis and pharmacological evaluation

C Pecoraro, M De Franco, D Carbone… - European Journal of …, 2023 - Elsevier
Among the different hallmarks of cancer, deregulation of cellular metabolism turned out to be
an essential mechanism in promoting cancer resistance and progression. The pyruvate …

[HTML][HTML] Discovery of the 3-amino-1, 2, 4-triazine-based library as selective PDK1 inhibitors with therapeutic potential in highly aggressive pancreatic ductal …

D Carbone, M De Franco, C Pecoraro… - International Journal of …, 2023 - mdpi.com
Pyruvate dehydrogenase kinases (PDKs) are serine/threonine kinases, that are directly
involved in altered cancer cell metabolism, resulting in cancer aggressiveness and …

Identification of novel piperazine-tethered phthalazines as selective CDK1 inhibitors endowed with in vitro anticancer activity toward the pancreatic cancer

L Akl, AA Abd El-Hafeez, TM Ibrahim, R Salem… - European Journal of …, 2022 - Elsevier
Pharmacologic inhibition of the oncogenic protein kinases using small molecules is a
promising strategy to combat several human malignancies. CDK1 is an example of such a …

Identification of novel pyruvate dehydrogenase kinase 1 (PDK1) inhibitors by kinase activity-based high-throughput screening for anticancer therapeutics

W Zhang, X Hu, H Chakravarty, Z Yang… - ACS combinatorial …, 2018 - ACS Publications
Warburg effect, a preference of aerobic glycolysis for energy production even in the
presence of adequate oxygen, is one of the most prominent distinctions of cancer cells from …

Identification of high-affinity inhibitors of pyruvate dehydrogenase kinase-3: towards therapeutic management of cancer

T Mohammad, K Arif, MF Alajmi, A Hussain… - Journal of …, 2021 - Taylor & Francis
Abstract Pyruvate dehydrogenase kinase 3 (PDK3) is a multifunctional enzyme that plays a
central role in the cancer metabolic switch by blocking pyruvate catabolism in the TCA cycle …

[HTML][HTML] Marine derived hamacanthins as lead for the development of novel PDGFRβ protein kinase inhibitors

B Pinchuk, E Johannes, S Gul, J Schlosser… - Marine Drugs, 2013 - mdpi.com
In this study, we report on pyrazin-2 (1 H)-ones as lead for the development of potent
adenosine triphosphate (ATP) competitive protein kinase inhibitors with implications as anti …

Anticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold

HSA Elzahabi, ES Nossier, NM Khalifa… - Journal of Enzyme …, 2018 - Taylor & Francis
An efficient synthesis of substituted pyrido [2, 3-d] pyrimidines was carried out and evaluated
for in vitro anticancer activity against five cancer cell lines, namely hepatic cancer (HepG-2) …

Discovery of 3, 6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico …

A Sabt, WM Eldehna, T Al-Warhi… - Journal of Enzyme …, 2020 - Taylor & Francis
Human health in the current medical era is facing numerous challenges, especially cancer.
So, the therapeutic arsenal for cancer should be unremittingly enriched with novel small …

Targeting the pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/PDK) axis to discover potent PDK inhibitors through structure-based virtual …

L Gan, Y Yang, Z Liang, M Zhang, Y He… - European Journal of …, 2024 - Elsevier
Proliferating cancer cells are characterized by the Warburg effect, a metabolic alteration in
which ATP is generated from cytoplasmic glycolysis instead of oxidative phosphorylation …