Thioamides in medicinal chemistry and as small molecule therapeutic agents

G Huang, T Cierpicki, J Grembecka - European Journal of Medicinal …, 2024 - Elsevier
Thioamides, which are fascinating isosteres of amides, have garnered significant attention in
drug discovery and medicinal chemistry programs, spanning peptides and small molecule …

Therapeutic approaches in pancreatic cancer: recent updates

L Kumar, S Kumar, K Sandeep, SKS Patel - Biomedicines, 2023 - mdpi.com
Cancer is a significant challenge for effective treatment due to its complex mechanism,
different progressing stages, and lack of adequate procedures for screening and …

Novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives as potential antitumor candidates targeting both EGFR and VEGFR-2; design, synthesis, biological …

SM Al-Muntaser, AA Al-Karmalawy, AM El-Naggar… - RSC …, 2023 - pubs.rsc.org
In this article, we continued our previous effort to develop new selective anticancer
candidates based on the basic pharmacophoric requirements of both EGFR and VEGFR-2 …

Anticancer evaluation and molecular docking of new pyridopyrazolo-triazine and pyridopyrazolo-triazole derivatives

MR Elmorsy, E Abdel-Latif, HE Gaffer, SE Mahmoud… - Scientific Reports, 2023 - nature.com
Amino-4, 6-dimethylpyrazolopyridine was applied as a precursor for the synthesis of some
new pyridopyrazolo-triazine and pyridopyrazolo-triazole derivatives through diazotization …

Deriving general structure–activity/selectivity relationship patterns for different subfamilies of cyclin-dependent kinase inhibitors using machine learning methods

S Kaveh, A Mani-Varnosfaderani, MS Neiband - Scientific Reports, 2024 - nature.com
Cyclin-dependent kinases (CDKs) play essential roles in regulating the cell cycle and are
among the most critical targets for cancer therapy and drug discovery. The primary objective …

NUSAP1 promotes pancreatic ductal adenocarcinoma progression by drives the epithelial-mesenchymal transition and reduces AMPK phosphorylation

Y Liu, R Tang, QC Meng, S Shi, J Xu, XJ Yu, B Zhang… - BMC cancer, 2024 - Springer
Background Pancreatic ductal adenocarcinoma (PDAC) has a poor prognosis, and its
molecular mechanisms are unclear. Nucleolar and spindle-associated protein 1 (NUSAP1) …

Multifunctional chitosan-bimetallic nanocarrier deliver 5-fluorouracil for enhanced treatment of pancreatic and triple-negative breast cancer

K Saravanakumar, A Sathiyaseelan… - International Journal of …, 2024 - Elsevier
This work aimed to prepare multifunctional aptamer-conjugated, photothermally responsive
5-fluorouracil (5fu)-loaded chitosan-bimetallic (Au/Pd) nanoparticles (APT-CS-5fu-Au/Pd …

Development of piperazine-and oxazine-linked pyrimidines as p65 subunit binders of NF–κB in human breast cancer cells

A Ravish, BC Narasimhachar, Z Xi, D Vishwanath… - Biomedicines, 2023 - mdpi.com
Nuclear factor kappa B (NF–κB) is a potential therapeutic target in breast cancer. In the
current study, a new class of oxazine–and piperazine–linked pyrimidines was developed as …

[HTML][HTML] Investigation of the relationship between COVID-19 and pancreatic cancer using bioinformatics and systems biology approaches

C Fang, H Sun, J Wen, X Wu, Q Wu, D Zhai - Medicine, 2024 - journals.lww.com
Background: The coronavirus disease 2019 (COVID-19) pandemic, caused by the severe
acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus, poses a huge threat to …

Synthesis of novel bioactive pyrido [2, 3-d] pyrimidine derivatives with potent cytotoxicity through apoptosis as PIM-1 kinase inhibitors

ES Tantawy, MS Nafie, HA Morsy, HA El-Sayed… - RSC …, 2024 - pubs.rsc.org
Direct synthesis and cytotoxicity activity of new series of pyrido [2, 3-d] pyrimidine was
described. Nicotinamide 2 was synthesized via cyclization of N-cyclohexyl derivative with …