6-Cinnamoyl-4-arylaminothienopyrimidines as highly potent cytotoxic agents: Design, synthesis and structure-activity relationship studies

M Toolabi, S Moghimi, TO Bakhshaiesh… - European journal of …, 2020 - Elsevier
In this paper, we described the synthesis and cytotoxic activities of two new series of thieno
[2, 3-d] pyrimidine and thieno [3, 2-d] pyrimidine derivatives. Most of the synthesized …

Quinoxaline‐based scaffolds targeting tyrosine kinases and their potential anticancer activity

AMS El Newahie, NSM Ismail… - Archiv der …, 2016 - Wiley Online Library
Quinoxaline derivatives, also called benzopyrazines, are an important class of heterocyclic
compounds. Quinoxalines have drawn great attention due to their wide spectrum of …

[HTML][HTML] Targeting kinases with anilinopyrimidines: discovery of N-phenyl-N'-[4-(pyrimidin-4-ylamino)phenyl]urea derivatives as selective inhibitors of class III …

V Gandin, A Ferrarese, M Dalla Via, C Marzano… - Scientific reports, 2015 - nature.com
Kinase inhibitors are attractive drugs/drug candidates for the treatment of cancer. The most
recent literature has highlighted the importance of multi target kinase inhibitors, although a …

The Story of Imatinib in GIST-a Journey through the Development of a Targeted Therapy

P Reichardt - Oncology Research and Treatment, 2018 - karger.com
The introduction of the tyrosine kinase inhibitor (TKI) imatinib 15 years ago has radically
changed the treatment of advanced/metastatic gastrointestinal stroma tumours (GIST). This …

[HTML][HTML] Targeting tyrosine kinases in ovarian cancer: small molecule inhibitor and monoclonal antibody, where are we now?

A Rendell, I Thomas-Bland, L McCuish, C Taylor… - Biomedicines, 2022 - mdpi.com
Ovarian cancer is one of the most lethal gynaecological malignancies worldwide. Despite
high success rates following first time treatment, this heterogenous disease is prone to …

[HTML][HTML] ROR1 is expressed in diffuse large B-cell lymphoma (DLBCL) and a small molecule inhibitor of ROR1 (KAN0441571C) induced apoptosis of lymphoma cells

A Ghaderi, AH Daneshmanesh, A Moshfegh… - Biomedicines, 2020 - mdpi.com
The receptor tyrosine kinase ROR1 is absent in most normal adult tissues, but
overexpressed in several malignancies. In this study, we explored clinical and functional …

[HTML][HTML] Brain metastases from NSCLC: radiation therapy in the era of targeted therapies

J Khalifa, A Amini, S Popat, LE Gaspar… - Journal of Thoracic …, 2016 - Elsevier
Brain metastases (BMs) will develop in a large proportion of patients with NSCLC
throughout the course of their disease. Among patients with NSCLC with oncogenic drivers …

Hydrogen Peroxide‐Inducible PROTACs for Targeted Protein Degradation in Cancer Cells

D Yu, H Fan, Z Zhou, Y Zhang, J Sun, L Wang… - …, 2023 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) provide a powerful technique to degrade
targeted proteins utilizing the cellular ubiquitin‐proteasome system. The major concern is …

Oligonucleotide aptamers against tyrosine kinase receptors: Prospect for anticancer applications

S Camorani, E Crescenzi, M Fedele… - Biochimica et Biophysica …, 2018 - Elsevier
Transmembrane receptor tyrosine kinases (RTKs) play crucial roles in cancer cell
proliferation, survival, migration and differentiation. Area of intense research is searching for …

[HTML][HTML] The proto-oncogene c-Kit inhibits tumor growth by behaving as a dependence receptor

H Wang, A Boussouar, L Mazelin… - Molecular cell, 2018 - cell.com
Summary c-Kit is a classic proto-oncogene either mutated or upregulated in cancer cells,
and this leads to its constitutive kinase activation and, thus, to uncontrolled proliferation …