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Comparative stability, toxicity and anti-leishmanial activity of triphenyl antimony(v) and bismuth(v) α-hydroxy carboxylato complexes†
Dalton Transactions ( IF 4 ) Pub Date : 2017-12-13 00:00:00 , DOI: 10.1039/c7dt04171c Rebekah N. Duffin 1, 2, 3, 4 , Victoria L. Blair 1, 2, 3, 4 , Lukasz Kedzierski 4, 5, 6 , Philip C. Andrews 1, 2, 3, 4
Dalton Transactions ( IF 4 ) Pub Date : 2017-12-13 00:00:00 , DOI: 10.1039/c7dt04171c Rebekah N. Duffin 1, 2, 3, 4 , Victoria L. Blair 1, 2, 3, 4 , Lukasz Kedzierski 4, 5, 6 , Philip C. Andrews 1, 2, 3, 4
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A series of triphenyl Sb(V) and Bi(V) α-hydroxy carboxylato complexes of the general formula [MPh3(O2CROH)2] and [MPh3(O2CRO)] have been successfully synthesised and characterised, and subsequently assayed for their comparative activity towards Leishmania parasites and human fibroblast cells. Four complexes are novel; [SbPh3Gly], [BiPh3(GlyH)2], [SbPh3(R-ManH)2] and [SbPh3(S-ManH)2], and have been structurally characterised through X-ray diffraction. These were combined in the study with the known complexes; ([SbPh3(R-Man)], [SbPh3(S-Man)], [BiPh3(R-ManH)2], [BiPh3(R-ManH)2], [SbPh3(BenzH)2], [BiPh3(BenzH)2], for which the crystal structures of [BiPh3(S-ManH)2] and [BiPh3(R-Man)2] have now been authenticated (GlyH2 = glycolic acid, R/S-ManH2 = mandelic acid, BenzH2 = benzilic acid). The complexes adopt a typical bipyramidal 7-coordinate geometry with the phenyl rings occupying the equatorial plane, and the ligands on the axial. In contrast to previous studies the Bi(V) compounds show a relatively high degree of stability in DMEM culture media. Promastigote and human fibroblast cell assays showed the Bi(V) analogues to be non-selectively toxic with a respective IC50 range of 3.58–6.33 μM and 5.83–7.01 μM. In contrast, the Sb(V) analogues provided much greater selectivity (promastigotes 12.5–20.7; fibroblasts 72.8–≥100 μM). Assessment of the Sb(V) complexes against amastigotes at 10 μM showed them to be effective with % infection values ranging from 9.5 ± 0.5–30 ± 1.3.
中文翻译：
三苯基锑（v）和铋（v）α-羟基羧基lato配合物的相对稳定性，毒性和抗利什曼活性†
已成功合成并表征了一系列通式为[MPh 3（O 2 CROH）2 ]和[MPh 3（O 2 CRO）]的三苯基Sb（V）和Bi（V）α-羟基羧基lato配合物，并进行了表征。随后测定其对利什曼原虫寄生虫和人成纤维细胞的比较活性。四个复合体是新奇的。[SbPh 3 Gly]，[BiPh 3（GlyH）2 ]，[SbPh 3（R -ManH）2 ]和[SbPh 3（S -ManH）2]，并且已通过X射线衍射对其进行了结构表征。在研究中将它们与已知的配合物结合在一起。（[[SbPh 3（R -Man ）]，[SbPh 3（S -Man ）]，[BiPh 3（R -ManH）2 ]，[BiPh 3（R -ManH）2 ]，[SbPh 3（BenzH）2 ]，[的BiPh 3（BenzH）2 ]中，其中[的BiPh晶体结构3（小号-ManH）2 ]和[的BiPh 3（ř -Man）2现在已经过鉴定]（GlyH 2 =乙醇酸，R / S -ManH 2 =扁桃酸，BenzH 2 =苯甲酸）。配合物采用典型的双锥体7坐标几何结构，其中苯环占据赤道平面，而配体在轴向上。与以前的研究相反，Bi（V）化合物在DMEM培养基中显示出相对较高的稳定性。前鞭毛体和人类成纤维细胞分析表明，Bi（V）类似物是非选择性毒性的，IC 50范围分别为3.58–6.33μM和5.83–7.01μM。相反，Sb（V）类似物提供更高的选择性（前鞭毛体12.5-20.7；成纤维细胞72.8-≥100μM）。对10μM的抗Amastigotes的Sb（V）复合物的评估表明，它们的感染百分比范围为9.5±0.5–30±1.3，非常有效。
更新日期：2017-12-13
中文翻译：
三苯基锑（v）和铋（v）α-羟基羧基lato配合物的相对稳定性，毒性和抗利什曼活性†
已成功合成并表征了一系列通式为[MPh 3（O 2 CROH）2 ]和[MPh 3（O 2 CRO）]的三苯基Sb（V）和Bi（V）α-羟基羧基lato配合物，并进行了表征。随后测定其对利什曼原虫寄生虫和人成纤维细胞的比较活性。四个复合体是新奇的。[SbPh 3 Gly]，[BiPh 3（GlyH）2 ]，[SbPh 3（R -ManH）2 ]和[SbPh 3（S -ManH）2]，并且已通过X射线衍射对其进行了结构表征。在研究中将它们与已知的配合物结合在一起。（[[SbPh 3（R -Man ）]，[SbPh 3（S -Man ）]，[BiPh 3（R -ManH）2 ]，[BiPh 3（R -ManH）2 ]，[SbPh 3（BenzH）2 ]，[的BiPh 3（BenzH）2 ]中，其中[的BiPh晶体结构3（小号-ManH）2 ]和[的BiPh 3（ř -Man）2现在已经过鉴定]（GlyH 2 =乙醇酸，R / S -ManH 2 =扁桃酸，BenzH 2 =苯甲酸）。配合物采用典型的双锥体7坐标几何结构，其中苯环占据赤道平面，而配体在轴向上。与以前的研究相反，Bi（V）化合物在DMEM培养基中显示出相对较高的稳定性。前鞭毛体和人类成纤维细胞分析表明，Bi（V）类似物是非选择性毒性的，IC 50范围分别为3.58–6.33μM和5.83–7.01μM。相反，Sb（V）类似物提供更高的选择性（前鞭毛体12.5-20.7；成纤维细胞72.8-≥100μM）。对10μM的抗Amastigotes的Sb（V）复合物的评估表明，它们的感染百分比范围为9.5±0.5–30±1.3，非常有效。
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