Synthesis and evaluation of anti-plasmodial and cytotoxic activities of epoxyazadiradione derivatives

A series of analogues were synthesised by modification of the key structural moieties of Epoxyazadiradione. Out of the library of all compounds tested, compounds 3c and 3g have showed potent anti-plasmodial activity against CQ-sensitive (IC50 2.8±0.29 μM and 1.5±0.01 μM) and CQ-resistant strains (IC50 1.4 ± μM and 1.2± 0.14), while compounds 3k, 3l and 3m showed modest activity against CQ-sensitive strain of P. falciparum with IC50 values of 2.3±0.4 μM, 2.9±0.1 μM and 1.7±0.06 μM, respectively.143