Synthesis and cancer cell cytotoxicity of water-soluble gold(III) substituted tetraarylporphyrin

The synthesis of novel substituted gold(III) tetraarylporphyrins with aqueous solubility has been carried out. The analogs ClAuTPP(CH3Py+·I−), ClAuTCPPNa, ClAuTPPCO2Na, ClAuTSPPNa and ClAuTPPNH2·HCl were evaluated for their in vitro cytotoxic activity against sarcoma 180 mouse tumor and SGC-7901 human gastric cancer cell line panel. Compound ClAuTCPPNa exhibited significant growth inhibitory properties against sarcoma 180 mouse tumor and SGC-7901 human gastric cancer cell examined, and afforded IC50 values < 25 μM for 66.63% of the cell lines in the panel. Compound ClAuTPPNH2·HCl was an effective inhibitor of sarcoma 180 mouse tumor and SGC-7901 human gastric cancer cell growth, but generally less effective as a cytotoxic agent. Thus, the substituted gold(III) porphyrin ClAuTCPP-Na+ and ClAuTPPNH2·HCl with aqueous solubility were regarded as useful lead compounds for further structural optimization.

The synthesis of several novel substituted gold(III) tetraarylporphyrins with aqueous solubility has been carried out. The new substituted gold(III) tetraarylporphyrins were evaluated for their in vitro cytotoxic activity against sarcoma 180 mouse and SGC-7901 human tumor cell line panel. Among them the substituted gold(III) porphyrin ClAuTCPP-Na+ and ClAuTPPNH2·HCl with aqueous solubility were regarded as useful lead compounds for further structural optimization.Figure optionsDownload as PowerPoint slideHighlights
► Substituted gold(III) tetraarylporphyrins with aqueous solubility were synthesized.
► Compounds were evaluated against sarcoma 180 and SGC-7901 cancer cells.
► ClAuTCPP-Na+ and ClAuTPPNH2·HCl were regarded as useful lead compounds.