Combining anti-cancer drugs with artificial sweeteners: Synthesis and anti-cancer activity of saccharinate (sac) and thiosaccharinate (tsac) complexes cis -[Pt(sac) 2 (NH 3 ) 2 ] and cis -[Pt(tsac) 2 (NH 3 ) 2 ]

Abstract

The new platinum(II) complexes cis-[Pt(sac)2(NH3)2] (sac=saccharinate) and cis-[Pt(tsac)2(NH3)2] (tsac=thiosaccharinate) have been prepared, the X-ray crystal structure of cis-[Pt(sac)2(NH3)2] x H2O reveals that both saccharinate anions are N-bound in a cis-arrangement being inequivalent in both the solid-state and in solution at room temperature. Preliminary anti-cancer activity has been assessed against A549 human alveolar type-II like cell lines with the thiosaccharinate complex showing good activity.

A comparative study of the coordination of saccharinate, thiosaccharinate and benzisothiozolinate ligands to cyclometalated [Pd(Me2NCH2C6H4-κN,C)(μ-Cl)]2: Molecular structures of [Pd(Me2NCH2C6H4-κN,C)(µ-X)]2 (X = sac, bit and tsac) and [Pd(Me2NCH2C6H4-κN,C)Cl(ampyH-κN)] (ampyH = 2-amino-3-methylpyridine)

“…The coordination chemistry of thiosaccharinate has also received recent attention [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18], but that of benzisothiozolinate (bit) remains virtually unexplored [19][20]…”

DNA/HSA Interactions and Anticancer Activity of a Palladium(II) Saccharinate Complex Bearing Ethyldiphenylphosphine

“…The anion has several coordination sites such as imino nitrogen, carbonyl and sulfonyl groups towards metal ions and undergoes complexation rather easily with a wide range of metal ions [5]. Mixed-ligand Pd(II) and Pt(II) sac complexes displayed significant anticancer activity [6][7][8][9][10][11]. Our research group has recently synthesized a number of Pd(II) and Pt(II) sac complexes containing mono and diphosphines.…”

Activation of thiosaccharin at a polynuclear osmium cluster

“…As a consequence, the coordination chemistry of the sac -1 has been extensively studied over the years [2,3]. In comparison, scant attention has been given to thiosaccharin (tsacH) which is closely related to sacH [3][4][5][6][7][8][9][10][11]. The heterocyclic compound tsacH can, in principle, exist in two, principle tautomeric forms in solution (Chart 1) that parallel the wellknown lactam ⇌ lactim equilibria established for dione-containing heterocycles.…”