ABSTRACT

Small molecule tyrosine kinase inhibitors of the epidermal growth receptor (EGF-R) are of pharmaceutical interest because these proteins kinases (PKs) are considered validated drug targets. In cancer, protein tyrosine kinase plays a key role in regulating numerous cellular functions including increased proliferation, decreased apoptosis, increased invasion, metastasis, and promote angiogenesis. Because signal transduction pathways are regulated in many tumor cells, targeting and inhibiting these kinases enzymes became attractive candidates for cancer therapy. The targeting of human epidermal growth factor receptor 2(HER2 or ErB-2/ neu) and epidermal growth factor receptor (EGFR or HER1-ErbB-1) by tyrosine kinase inhibitors (KIs) represent one such therapeutic approach. The new novel 2-[4-(amino-1-yl)but-2-yn]-1,2,3,4-tetrahydroisoquinoline (ZI 1-6) provide effective overlap with (EGFR or HER2) through ionic, hydrogen bonding, charge transfer and hydrophobicity. These speculations are supported by molecular docking, structural elucidation were consistent with IR, NMR, and elemental analysis of the prepared compounds. Keywords: Tetrahydroisoquinoline; Alkylation; Mannich reaction; Molecular docking

https://ijbpas.com/pdf/2019/May/MS_IJBPAS_2019_4703.pdf

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https://doi.org/10.31032/IJBPAS/2019/8.5.4703