New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease

Incorporating Selenium into Heterocycles and Natural Products─From Chemical Properties to Pharmacological Activities

“…Phenolic selenosemicarbazone 8c13 (EC 50 = 4.87 μM) presents more potent antioxidant activity than the naturally occurring compound hydroxytyrosol (EC 50 = 13.80 μM), an antioxidant in olive oil, while 8c14 shows low micromolar inhibitory activity against a panel of cancer cell lines, including A549, HBL-100, HeLa, SW1573, T-47D, and WiDr (GI 50 = 1.1–3.2 μM). Selenosemicarbazone 8c15 (10 mg/kg bw/day) reduced the parasitemia profile by 50% in a murine model of acute Chagas disease . Selenoureido benzenesulfonamide 8c16 displayed low nanomolar inhibitory activity against a panel of hCA isoforms, hCA I ( K i = 85.7 nM), hCA II ( K i = 0.7 nM), hCA VII ( K i = 1.7 nM), and hCA IX ( K i = 3.5 nM) .…”

“…Selenosemicarbazone 8c15 (10 mg/kg bw/day) reduced the parasitemia profile by 50% in a murine model of acute Chagas disease. 87 Selenoureido benzenesulfonamide 8c16 displayed low nanomolar inhibitory activity against a panel of hCA isoforms, hCA I (K i = 85.7 nM), hCA II (K i = 0.7 nM), hCA VII (K i = 1.7 nM), and hCA IX (K i = 3.5 nM). 88 Considering the synergistic antioxidant properties of Se and the sulfonamide pharmacophore, 8c16 may have the potential to inhibit cancer cell overexpression in certain CAs while the redox state is impaired.…”

Acylselenoureas, selenosemicarbazones and selenocarbamate esters: Versatile ligands in coordination chemistry

“…Several groups have studied the activity of 2-pyridyl-derived selenosemicarbazones as well as their metal complexes against Chagas disease and malaria. [117][118][119][120][121] The coordination chemistry and biological activity of metal complexes containing selenosemicarbazones derived from 2-acetylpyridine (HSeL acpy ) have been investigated in some detail over the years. Structural diversity can be increased by varying the substituents on the nitrogen atom at the 4-position.…”