Synthesis, characterization, and in vitro cytotoxicity of some gold(I) and trans platinum(II) thionate complexes containing water-soluble PTA and DAPTA ligands. X-ray crystal structures of [Au(SC4H3N2)(PTA)], trans-[Pt(SC4H3N2)2(PTA)2], trans-[Pt(SC5H4N)2(PTA)2], and trans-[Pt(SC5H4N)2(DAPTA)2].
A series of gold(I) and platinum(II) complexes of the type [Au(SR)(P)] and trans-[Pt(SR) 2(P) 2] [SR = 2-thiopyridine (SPy), 2-thiopyrimidine (SPyrim); P = 1,3,5-triaza-7-phosphaadamantane (PTA), 3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane (DAPTA)] were prepared and characterized, and their in vitro cytotoxicities against a panel of seven human cancer cell lines were evaluated. The highly water soluble gold(I) complexes [Au(SR)(P)] [P = PTA and SR = SPy ( 1), SPyrim ( 2); P = DAPTA and SR = SPy ( 3), SPyrim ( 4)] showed low cytotoxicity, while the platinum(II) complexes trans-[Pt(SR) 2(P) 2] [P = PTA and SR = SPyrim ( 5), SPy ( 6); P = DAPTA and SR = SPyrim ( 7), SPy ( 8)] demonstrated potent cytotoxicity for ovarian, colon, renal, and melanoma cancer cell lines on the basis of a comparison with ID 50 values for some established cytotoxic drugs. Single crystals of 2, 5, 6, and 8 suitable for X-ray structural characterization were obtained, and the study revealed the trans configuration for 5, 6, and 8 in their solid states.
Miranda
Susana
S
Departamento de Química, Facultad de Ciencias, Universidad de Burgos, 09001 Burgos, Spain.
Vergara
Elena
E
Mohr
Fabian
F
de Vos
Dick
D
Cerrada
Elena
E
Mendía
Aránzazu
A
Laguna
Mariano
M
D000218:Adamantane / Q000031:analogs & derivatives; D000970:Antineoplastic Agents / Q000737:chemistry*; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006046:Gold; D006801:Humans; D008024:Ligands; D009942:Organometallic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D009943:Organophosphorus Compounds; D009944:Organoplatinum Compounds / Q000737:chemistry / Q000494:pharmacology; D012995:Solubility; D013329:Structure-Activity Relationship
C501763:1,3,5-triaza-7-phosphaadamantane; D000970:Antineoplastic Agents; D008024:Ligands; D009942:Organometallic Compounds; D009943:Organophosphorus Compounds; D009944:Organoplatinum Compounds; D006046:Gold; D000218:Adamantane