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• W4200422997 endingPage "115627" @default.
• W4200422997 startingPage "115627" @default.
• W4200422997 abstract "A change in the aryl group of Sb(V) complexes has an influence on their anti-leishmanial activity. Tolyl complexes are the most toxic, but also the most active against L. major . Tris (5-bromo-2-methoxyphenyl)antimony shows the least toxicity and higher selectivity for parasite cells. • Synthesis of tris -arylantimony dicarboxylates by oxidative addition reaction. • Intermolecular interactions involving halogen atoms. • Impact of varying the aryl groups on anti-leishmanial activity and cytotoxicity. • Higher lipophilicity induces better biological activity and higher toxicity. Five tris -arylantimony bis (pentafluoropropionates) of the general formula Ar 3 Sb[ OC ( O ) CF 2 CF 3 ] 2 with Ar = Ph ( 1 ), m -Tol, ( 2 ) p -Tol ( 3 ), C 6 H 4 F-4 ( 4 ), C 6 H 3 -OMe-2-Br-5 ( 5 ) have been synthesized by an oxidative addition reaction. Four of them ( 1 – 3 , 5 ) are structurally novel. All structures were analytically characterized by X-ray diffraction, IR, 1 H, 13 C and 19 F NMR spectroscopy. The solid-state structures determined by X-ray diffraction analysis have shown that the antimony centre has a typical trigonal–bipyramidal geometry with carboxylic oxygen atoms in axial positions and carbon atoms of aryl groups in the equatorial plane. All complexes have been screened for their anti-leishmanial activity and cytotoxicity towards mammalian macrophages. IC 50 values are found in the ranges of 2.32–28.7 μM for the promastigote assay, and 5.14–41.6 μM for the macrophages. Two complexes with the selectivity indices SI = 2.49 ( 2 ) and 3.75 ( 5 ) have been assessed for their anti-amastigote activity. The percentage infection values of 10.00 % ± 2.25 ( 2 ) and 27.50 % ± 2.94 ( 5 ) are obtained, showcasing the need for further investigations into a change in aryl group and the structure activity relationships it presents." @default.
• W4200422997 created "2021-12-31" @default.
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• W4200422997 date "2022-02-01" @default.
• W4200422997 modified "2023-09-30" @default.
• W4200422997 title "Investigations into a change of aryl group on the cytotoxicity and anti-leishmanial activity of a series of tris-aryl Sb(V) pentafluoropropionates" @default.
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• W4200422997 doi "https://doi.org/10.1016/j.poly.2021.115627" @default.
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