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 …
KRAS G12D inhibitors via combinatorial virtual screening approach. Most compounds …
Prospects of targeting PI3K/AKT/mTOR pathway in pancreatic cancer
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 …
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
In contrast to mitochondria in healthy cells, which utilize oxidative phosphorylation,
malignant cells undergo elevated glycolysis for energy production using glucose. The …
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 …
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
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) …
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
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 …
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] …
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
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 …
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?
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 …
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 …
cancers in humans, due to late diagnosis and limited treatment possibilities. Improved …