Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy

A Ayati, S Moghimi, M Toolabi, A Foroumadi - European Journal of …, 2021 - Elsevier
Despite significant improvements of new treatment options, cancer continues to represent as
one of the most common and fatal disease. The EGFR signaling pathway is considered as a …

Current advances of tubulin inhibitors as dual acting small molecules for cancer therapy

KE Arnst, S Banerjee, H Chen, S Deng… - Medicinal research …, 2019 - Wiley Online Library
Microtubule (MT)‐targeting agents are highly successful drugs as chemotherapeutic agents,
and this is attributed to their ability to target MT dynamics and interfere with critical cellular …

Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2-d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule …

R Romagnoli, F Prencipe, P Oliva… - Journal of Medicinal …, 2019 - ACS Publications
The clinical evidence for the success of tyrosine kinase inhibitors in combination with
microtubule-targeting agents prompted us to design and develop single agents that possess …

A review on fused pyrimidine systems as EGFR inhibitors and their structure–activity relationship

TT Yadav, G Moin Shaikh, MS Kumar… - Frontiers in …, 2022 - frontiersin.org
Epidermal growth factor receptor (EGFR) belongs to the family of tyrosine kinase that is
activated when a specific ligand binds to it. The EGFR plays a vital role in the cellular …

Furo[2,3‐d]pyrimidines as Mackinazolinone/Isaindigotone Analogs: Synthesis, Modification, Antitumor Activity, and Molecular Docking Study

B Song, L Nie, K Bozorov, C Niu… - Chemistry & …, 2023 - Wiley Online Library
The chemical transformation of the tricyclic furo [2, 3‐d] pyrimidines was performed under
isosteric and scaffold‐hopping strategies focusing on the synthesis of its arylidene and imine …

Pd(II)-Catalyzed Three-Component Synthesis of Furo[2,3-d]pyrimidines from β-Ketodinitriles, Boronic Acids, and Aldehydes

HN Dhara, B Das, D Barik, S Manna, BK Patel - Organic Letters, 2023 - ACS Publications
A Pd (II)-catalyzed three-component synthesis of 2, 4, 6-triarylfuro [2, 3-d] pyrimidines from β-
ketodinitriles, boronic acids, and aldehydes has been developed. The participation of both …

Synthesis and anticancer activities of diverse furo[2,3-d]pyrimidine and benzofuro[3,2-d]pyrimidine derivatives

X Tang, A Zheng, F Wu, C Liao, Y Hu… - Synthetic …, 2022 - Taylor & Francis
A series of diverse furo [2, 3-d] pyrimidines (2a–2b, 4a–4d and 8a–8c) and benzofuro [3, 2-d]
pyrimidines (12a–12c) were synthesized and screened for their antitumor effects against …

Coumarin–furo [2, 3-d] pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies

T Wang, Y Gao, F Wu, L Luo, J Ma, Y Hu - RSC Medicinal Chemistry, 2024 - pubs.rsc.org
The design, synthesis and investigation of antitumor activities of some coumarin–furo [2, 3-d]
pyrimidone hybrid molecules are reported. In vitro, HepG2 cells were used to investigate the …

Copper (II) mediated C–H methylthiolation of 2-phenyl pyridines with dimethyl sulfoxide using an amino acid ligand

Y Xiao, S Wang, J Liu, H Zhang, Y Xu - Tetrahedron Letters, 2019 - Elsevier
A novel protocol for the C–H methylthiolation of 2-phenyl pyridines using DMSO as the
methylthio source and an amino acid ligand is described. This simple procedure requires …

Radiosynthesis and evaluation of [11C] AG-488, a dual anti-angiogenetic and anti-tubulin PET ligand

JSD Kumar, A Molotkov, P Carberry, T Chaly… - Bioorganic & Medicinal …, 2022 - Elsevier
Combinations of antiangiogenic and cytotoxic agents show promising results in the
treatment of cancer. However, there is a lack of single agent with both antiangiogenic and …