Discovery of Thieno [2, 3-d] pyrimidine-based KRAS G12D inhibitors as potential anticancer agents via combinatorial virtual screening

L Li, J Liu, Z Yang, H Zhao, B Deng, Y Ren… - European Journal of …, 2022 - Elsevier
A series of novel thieno [2, 3-d] pyrimidine analogs were designed and synthesized as
KRAS G12D inhibitors via combinatorial virtual screening approach. Most compounds …

Prospects of targeting PI3K/AKT/mTOR pathway in pancreatic cancer

M Mortazavi, F Moosavi, M Martini, E Giovannetti… - Critical reviews in …, 2022 - Elsevier
Pancreatic ductal adenocarcinoma (PDAC) has one of the worst prognoses among all
malignancies. PI3K/AKT/mTOR signaling pathway, a main downstream effector of KRAS is …

[HTML][HTML] Expression of pyruvate dehydrogenase kinase-1 in gastric cancer as a potential therapeutic target

H Hur, Y Xuan, YB Kim, G Lee… - International …, 2013 - spandidos-publications.com
In contrast to mitochondria in healthy cells, which utilize oxidative phosphorylation,
malignant cells undergo elevated glycolysis for energy production using glucose. The …

Targeting PDK1 in cancer

C Raimondi, M Falasca - Current medicinal chemistry, 2011 - ingentaconnect.com
Abnormal activation of phosphoinositide 3-kinase (PI3K) signalling is very common in
cancer, leading to deregulation of several intracellular processes normally controlled by this …

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) …

Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors

YD Gao, D Feng, RP Sheridan, G Scapin… - Bioorganic & medicinal …, 2007 - Elsevier
Molecular modeling was used to improve potency of the cyclohexylamine series. In addition,
a 3-D QSAR method was used to gain insight for reducing off-target DPP-8/9 activities …

[HTML][HTML] Discovery of pyrazolo [3, 4-d] pyrimidine and pyrazolo [4, 3-e][1, 2, 4] triazolo [1, 5-c] pyrimidine derivatives as novel CDK2 inhibitors: synthesis, biological and …

IF Nassar, MTA Aal, WA El-Sayed, MAE Shahin… - RSC …, 2022 - pubs.rsc.org
CDK2 inhibition is an appealing target for cancer treatment that targets tumor cells in a
selective manner. A new set of small molecules featuring the privileged pyrazolo [3, 4-d] …

[HTML][HTML] Discovery of Hordenine as a potential inhibitor of pyruvate dehydrogenase kinase 3: implication in lung Cancer therapy

S Anwar, T Mohammad, A Shamsi, A Queen… - Biomedicines, 2020 - mdpi.com
Design and development of potential pyruvate dehydrogenase kinase 3 (PDK3) inhibitors
have gained attention because of their possible therapeutic uses in lung cancer therapy. In …

[HTML][HTML] Targeting tumor metabolism for cancer treatment: is pyruvate dehydrogenase kinases (PDKs) a viable anticancer target?

W Zhang, SL Zhang, X Hu, KY Tam - International journal of …, 2015 - ncbi.nlm.nih.gov
Cancer remains a lethal threat to global lives. Development of novel anticancer therapeutics
is still a challenge to scientists in the field of biomedicine. In cancer cells, the metabolic …

[HTML][HTML] Cyclin dependent kinase-1 (CDK-1) inhibition as a novel therapeutic strategy against pancreatic ductal adenocarcinoma (PDAC)

R Wijnen, C Pecoraro, D Carbone, H Fiuji, A Avan… - Cancers, 2021 - mdpi.com
Simple Summary Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal
cancers in humans, due to late diagnosis and limited treatment possibilities. Improved …