Synthesis of new 1,3,4-oxadiazole-1,4-benzoxazinone hybrids as tubulin polymerization inhibiting anticancer agents and their in silico studies

Abstract

Herein, we synthesized some new 1,3,4-oxadiazole-1,4-benzoxazinone hybrids (7a-7n) and evaluated for their in vitro anticancer potency towards A549 (lung), MCF-7 (breast) and HeLa (cervicl) cancer cell lines. Amongst series (7a-7n), compound 7d had greater potency against all cell lines than the standard nocodazole with IC50 ranging from 0.3 ± 0.07 to 0.9 ± 0.16 μM. Compounds 7j and 7l have also shown superior potency against A549 (lung) and most promising potency against MCF-7 (breast) as compared to positive control. Further, compounds 7d and 7j were found to be 2 to 3 times more potent in in vitro tubulin polymerization inhibition than the standard CA-4. Finally, the results of in silico studies were also supporting the corresponding in vitro anticancer activity and tubulin polymerization inhibition data of compounds 7d, 7j and 7l.