Novel quinazolinone‐triazole hybrid heterocycles were identified as cytotoxic agents to inhibit glioblastoma cell proliferation. These compounds were synthesized using click reaction by building a triazole linker on quinazolinone and tested for cytotoxicity on C6 glioma cell lines, a facsimile of glioblastoma multiforme. Few of these series significantly reduced the proliferation of cell lines with IC50 8–15 μM and may act as fetching leads for glioblastoma therapies. The binding affinity and ligand‐receptor interaction between hybrids and rat thymidylate synthase were investigated using molecular docking techniques.

A Cu(II)-catalyzed Csp2-Se and Csp2-Sulfur bond formation was achieved with moderate to good yields without the aid of Lewis acid and base. The reaction is compatible with a wide range of heterocycles such as benzothiazole, thiazole, and imidazole. Also, this typical protocol is found to be active in thio-selenation via S-H activation. Additionally, we proposed a plausible mechanistic pathway involving Cu(III) putative intermediate.

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Herein, we report a series of 1,2,3-triazole combined with quinazoline hybrid heterocyclic compounds by 1,3-dipolar cycloaddition reaction catalyzed by Cu(I). This reaction has been carried out between quinazoline based alkyne and aryl/benzyl azides under optimized conditions. Modification of 4-hydroxyquinazoline by propargyl bromide in presence of potassium carbonate gives a corresponding alkyne. Structure of the synthesized compounds has been characterized by IR, 1 H, and 13 C NMR, ESI-Mass, and HRMS spectra. The products have been tested for anticancer activity against C6 glioma cell lines and characterized by moderate cytotoxic activity.