title: Synthesis and cancer cell cytotoxicity of water-soluble gold(III) substituted tetraarylporphyrin.
abstract: The synthesis of novel substituted gold(III) tetraarylporphyrins with aqueous solubility has been carried out. The analogs ClAuTPP(CH(3)Py(+)·I(-)), ClAuTCPPNa, ClAuTPPCO(2)Na, ClAuTSPPNa and ClAuTPPNH(2)·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 IC(50) values <25 μM for 66.63% of the cell lines in the panel. Compound ClAuTPPNH(2)·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 ClAuTPPNH(2)·HCl with aqueous solubility were regarded as useful lead compounds for further structural optimization.
authors.affiliation: School of Chemistry and Chemical Engineering, Yangzhou University, Yangzhou, PR China.
authors.forename: Liang
authors.initials: L
authors.lastname: Sun
authors.forename: Huasheng
authors.initials: H
authors.lastname: Chen
authors.forename: Zonglei
authors.initials: Z
authors.lastname: Zhang
authors.forename: Qian
authors.initials: Q
authors.lastname: Yang
authors.forename: Haibo
authors.initials: H
authors.lastname: Tong
authors.forename: Aihua
authors.initials: A
authors.lastname: Xu
authors.forename: Cunde
authors.initials: C
authors.lastname: Wang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006046:Gold / Q000737:chemistry*; D006801:Humans; D051379:Mice; D011166:Porphyrins / Q000737:chemistry*; D012995:Solubility; D013329:Structure-Activity Relationship; D014867:Water / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D011166:Porphyrins; D014867:Water; D006046:Gold