Design and synthesis of novel sulphamide tethered quinazolinone hybrids as potential antitumor agents

In an attempt to develop potential and selective antitumor agents, a series of novel sulphamide tethered quinazolinone hybrids were efficiently synthesized and evaluated for antitumor activity against four cancer cell lines such as HeLa (cervical), MDA-MB-231 (breast), PANC-1 (pancreatic), and A549 (lung) in vitro. All the compounds (5a-j, 6a-g) exhibited significant anti-proliferative activity with GI50 values ranging from 0.045 to 6.94 μM, while compound 10c showed potent activity against all the cell lines (He La, MDA-MB-231, PANC-1 and A549) with GI50 values ranging from 0.09 to 0.21 μM. We have explored the binding mode and key active site interactions in HDAC8 and EHMT2 proteins. The docking results are complementary to the experimental results.