Click chemistry based synthesis, cytotoxic activity and molecular docking of novel triazole-thienopyrimidine hybrid glycosides targeting EGFR

Abstract

Click chemistry based synthesis, cytotoxic activity and molecular docking of novel triazolethienopyrimidine hybrid glycosides targeting EGFR,

1,2,3‐Triazole hybrids as anticancer agents: A review

“…[105] Rezki et al [106] have synthesized benzothiazole/isatin linked to a 1,2, gefitinib. [107] The phthalimide scaffold linked to 1,2,3-triazole (114) showed selectivity and the most potent cytotoxic activity on MCF- which was similar to the interaction of reference drug erlotinib. This proves the role of the triazole fragment in inhibiting EGFR for anticancer therapy [108] (Figure 9).…”

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

“…10,11 As a result, international recommendations advocate anti-EGFR medicines as the rst-line treatment in patients with advanced EGFR mutations, due to their higher efficacy and safety compared to standard chemotherapy. 9,12,13 Furthermore, vascular endothelial growth factor receptor-2 (VEGFR-2), a transmembrane tyrosine kinase receptor, has been has been identied as the most important factor in inducing angiogenesis, [14][15][16] which is considered as one of the dening features of tumor growth, invasion and metastasis. VEGFR-2 has long been recognized as the most important target in cancer anti-angiogenesis therapy.…”

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

“…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.…”

“…1,2,3-Triazole motifs are known to be present in a large number of compounds exhibiting anticancer [ 33 ] and anti-HIV [ 34 , 35 ] activity in addition to their ability to be potent pharmacophores [ 36 , 37 ]. Compounds possessing triazole scaffold V and VI revealed remarkable in vitro cytotoxicity against different human cancer cell lines via a significant inhibition of EGFR [ 8 ] ( Figure 1 ). Furthermore, tetrazole, being a possible bioisoster of 1,2,3-triazole with a five-membered heterocyclic structure, has been exhibited by its derivatives anticancer [ 38 , 39 ], antibacterial [ 40 , 41 ], antifungal [ 42 , 43 ], antimalarial [ 44 , 45 ], antitubercular [ 46 , 47 ] activities.…”