Identification of novel quinazolinone hybrids as cytotoxic agents against C6 glioma cell lines

Abstract

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.

Synthetic miR-21 decoy circularized by tRNA splicing mechanism inhibited tumorigenesis in glioblastoma in vitro and in vivo models

“…To confirm that our designed miR-21 decoys had therapeutic effects in vivo , we used C6 cells, which are a facsimile of GBM with a relative gene expression pattern. 47 Our findings indicate that CM21D and LM21D could significantly decrease tumor volume, and the repression effect of CM21D was more evident than that of the linear form. This finding confirms the stability and efficiency of CM21D compared with LM21D.…”

Design, Synthesis of Novel 1,2,3‐Triazole Pendent Quinazolinones and Their Cytotoxicity against MCF‐7 Cell Line

“…[40] Several quinazolinone -1,2,3-triazole hybrids are reported in the literature which are eventually produced significant pharmacological activities such as phosphoinositide 3-kinase inhibition, [41] α-glucosidase inhibition, [42] lipoxygenase inhibition [43] antitubercular, [44] antibacterial [45] and anticancer activities. [46] Our research group recently published the anticancer activity of hybrid compounds in which triazole tethered at 2-position of quinazolinone against C6 glioma cell lines [47] and other bio-active hybrids containing quinazolines -triazoles with methoxy linkers as anti-cancer agents and kinase inhibitors. [48] Inspired by the important biological activities of quinazolinones, 1,2,3triazoles and their hybrids, and extension to our previous work, [49] we have designed and synthesised a novel series of 1,2,3-triazole pendent quinazolinone analogous with methylamino linker (Figure 2).…”