Herein, we report the synthesis of 12 new naphthoquinone derivatives, 6 substituted 1,4-naphthoquinones and 6 heterocycle-fused naphthoquinones, as well as evaluation of their trypanocidal and leishmanicidal activities. Compounds 11a and 13a were active against the amastigote stage of T. cruzi and showed low cytotoxic effects. With respect to leishmanicidal assays, all compounds were inactive against the promastigote stages of L. chagasi and L. braziliensis.

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This paper reports the synthesis of methanones and esters bearing different substitution patterns as spacer groups between aromatic rings. This series of compounds can be considered phenstatin analogs. Two of the newly synthesized compounds, 5a and 5c, strongly inhibited tubulin polymerization and the binding of [3H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bind to tubulin at the colchicine site.