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 <25μM 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.