Unveiling the potential of isatin-grafted phenyl-1, 2, 3-triazole derivatives as dual VEGFR-2/STAT-3 inhibitors: Design, synthesis and biological assessments
The use of VEGFR-2 inhibitors as a stand-alone treatment has proven to be ineffective in
clinical trials due to the robustness of cellular response loops that lead to treatment …
clinical trials due to the robustness of cellular response loops that lead to treatment …
Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In …
SM Hefny, TF El-Moselhy, N El-Din… - Journal of Medicinal …, 2024 - ACS Publications
A dual-targeting approach is predicted to yield better cancer therapy outcomes.
Consequently, a series of coumarin-based thiazoles (5a–h, 6, and 7a–e) were designed and …
Consequently, a series of coumarin-based thiazoles (5a–h, 6, and 7a–e) were designed and …
Pyrimidine-based dual-target inhibitors targeting epidermal growth factor receptor for overcoming drug resistance in cancer therapy (2006-present)
Y An, X Lv, S Xu, H Li, P Zheng, W Zhu… - European Journal of …, 2025 - Elsevier
The epidermal growth factor receptor (EGFR) is a pivotal member of the epidermal growth
factor receptor family, exerting crucial regulatory influence on cellular physiological …
factor receptor family, exerting crucial regulatory influence on cellular physiological …
Development of new LSM-83177 analogues as anti-tumor agents against colorectal cancer targeting p53-MDM2 interaction
LSM-83177, a phenoxy acetic acid derivative, is a small molecule reported for its promising
anti-tumor properties. Via inhibiting the interaction between MDM2 and p53, LSM-83177 can …
anti-tumor properties. Via inhibiting the interaction between MDM2 and p53, LSM-83177 can …
Muti-target rationale design of novel substituted N-phenyl-2-((6-phenylpyridazin-3-yl) thio) acetamide candidates as telomerase/JAK1/STAT3/TLR4 inhibitors: In vitro …
In this work, additional effort was applied to design new BIBR1532-based analogues with
potential inhibitory activity against telomerase and acting as multitarget antitumor candidates …
potential inhibitory activity against telomerase and acting as multitarget antitumor candidates …
Fragment-based design and synthesis of coumarin-based thiazoles as dual c-MET/STAT-3 inhibitors for potential antitumor agents
Abstract c-MET and STAT-3 are significant targets for cancer treatments. Here, we describe
a class of very effective dual STAT-3 and c-MET inhibitors with coumarin-based thiazoles …
a class of very effective dual STAT-3 and c-MET inhibitors with coumarin-based thiazoles …
Novel sulfonamide-tethered Schiff bases as anti-proliferative agents with VEGFR-2 inhibitory activity: Synthesis, biological assessment, and molecular dynamic …
Schiff bases tethered with sulfonamide functionality (6a-l) are reported as potential
anticancer agents and apoptotic inducers. The anti-proliferative activities of the tested Schiff …
anticancer agents and apoptotic inducers. The anti-proliferative activities of the tested Schiff …
Discovery of new 1, 3-diphenylurea appended aryl pyridine derivatives as apoptosis inducers through c-MET and VEGFR-2 inhibition: design, synthesis, in vivo and in …
Interest has been generated in VEGFR-2 and c-MET as potential receptors for the treatment
of different malignancies. Using aryl pyridine derivatives with 1, 3-diphenylurea attached, a …
of different malignancies. Using aryl pyridine derivatives with 1, 3-diphenylurea attached, a …
Exploring antitumor activity of novel imidazo [2, 1-b] thiazole and imidazo [1, 2-a] pyridine derivatives on MDA-MB-231 cell line: Targeting VEGFR-2 enzyme with …
Our study explored the anticancer potential of novel heterocyclic compounds, specifically 6a-
d, 8a-d, 12a-d, and 13a-d, which are derived from imidazo [2, 1-b] thiazole and imidazo [1, 2 …
d, 8a-d, 12a-d, and 13a-d, which are derived from imidazo [2, 1-b] thiazole and imidazo [1, 2 …
A new framework for novel analogues of pazopanib as potent and selective human carbonic anhydrase inhibitors: Design, repurposing rational, synthesis …
SM Hefny, TF El-Moselhy, N El-Din, A Ammara… - European Journal of …, 2024 - Elsevier
Herein, we describe the design and synthesis of novel aryl pyrimidine benzenesulfonamides
APBSs 5a-n, 6a-c, 7a-b, and 8 as pazopanib analogues to explore new potent and selective …
APBSs 5a-n, 6a-c, 7a-b, and 8 as pazopanib analogues to explore new potent and selective …