Novel benzothiazole hybrids targeting EGFR: Design, synthesis, biological evaluation and molecular docking studies

Quercetin Hybrids—Synthesis, Spectral Characterization and Radical Scavenging Potential

“…Certainly, 2-substituted derivatives of benzothiazole and benzimidazole are important biologically active compounds with diverse medicinal applications [21][22][23]. Furthermore, the synthesis of hybrid molecules containing two pharmacophore fragments and their evaluation as potent drug candidates have been under constant escalation for the last two decades [24,25]. Additionally, the radical scavenging assays of the new synthetic compounds have been consummated to analyze their effectiveness as antioxidant agents.…”

Synthesis and biological evaluation of new derivatives of thieno-thiazole and dihydrothiazolo-thiazole scaffolds integrated with a pyrazoline nucleus as anticancer and multi-targeting kinase inhibitors

“…The most active cytotoxic agents 1, 3c were also evaluated as multitargeted protein kinases against EGFR, VEGFR-2 and BRAF V600E tyrosine kinases and sorafenib was used as a positive control. 61,62 The obtained results were summarized in Table 2 . A significant sensitivity was detected by EGFR kinase against both compounds 1, 3c which revealed a near equipotent or slightly higher inhibitory activity than that of the reference drug sorafenib with IC 50 s ; 0.022, 0.017 μM, respectively, while IC 50 sorafenib ; 0.025 μM.…”

“…The most active cytotoxic compounds that showed promising IC 50 values against 1, 3c were further examined for their inhibitory activities against EGFR, VEGFR-2 and BRAF V600E . 61–63 More details in the ESI. †…”

Novel 1,2,3-Triazole-Coumarin Hybrid Glycosides and Their Tetrazolyl Analogues: Design, Anticancer Evaluation and Molecular Docking Targeting EGFR, VEGFR-2 and CDK-2

“…One of the most prominent oncogenic kinases is epidermal growth factor receptor (EGFR), which is a receptor tyrosine kinase and plays an essential mediating role in cell proliferation, angiogenesis, apoptosis and metastatic spread [ 5 ]. It is overexpressed in a multiplicity of human cancers, including breast, colorectal, lung, prostate, ovary and pancreatic cancers [ 6 , 7 ].…”

“…It is overexpressed in a multiplicity of human cancers, including breast, colorectal, lung, prostate, ovary and pancreatic cancers [ 6 , 7 ]. Poor treatment outcomes as a result of resistance to radiotherapy, hormone therapy, and cytotoxic drugs presented an opportunity for anti-EGFR drug recommendations due to their higher safety and efficacy compared to standard chemotherapy [ 5 , 8 , 9 ]. Moreover, vascular endothelial growth factor receptor-2 (VEGFR-2) has a crucial role in the induction of angiogenesis [ 10 , 11 , 12 ], which is correlated with tumour growth, invasion and metastasis.…”