Products Cited in Publications Worldwide A Click Synthesis, Molecular Docking and Biological Evaluation of 1,2,3-triazoles-benzoxazepine hybrid as potential anticancer agents

A Click Synthesis, Molecular Docking and Biological Evaluation of 1,2,3-triazoles-benzoxazepine hybrid as potential anticancer agents

Ashram, Muhammad; Habashneh, Almeqdad Y.; Bardaweel, Sanaa; Taha, Mutasem O.

DOI:

Abstract

A series of novel 1,2,3-triazole-benzoxazepine hybrid molecules were synthesized and evaluated for their anticancer properties against four cancer cell lines (Caco-2, PC3, MCF-7, and HL60). Most of the synthesized compounds exhibited moderate to good cytotoxicity against tested cancer cell lines. Three of the prepared compounds, namely, 2, 3, and 4, showed excellent anticancer properties with micromolar IC50 values ranging from 6 to 18 μM. In silico pharmacophore profiling followed by in-vitro enzyme assays showed 2, 3, and 4 to have micromolar inhibitory IC50 values against the oncogenic kinase FLT3. These compounds represent new inhibitory leads of novel chemotypes against FLT3.

Keywords

Benzoxazepines ; 1, 2, 3-Triazoles ; Anticancer agents ; In vitro bioassay ; Docking study

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2,4-Dihydroxybenzaldehyde

A24505295-01-298%

2,4-Dihydroxybenzaldehyde

12.0/10g

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