Miranda Susana, Vergara Elena, Mohr Fabian, de Vos Dick, Cerrada Elena, Mendía Aránzazu, Laguna Mariano
Departamento de Química, Facultad de Ciencias, Universidad de Burgos, 09001 Burgos, Spain.
Inorg Chem. 2008 Jul 7;47(13):5641-8. doi: 10.1021/ic7021903. Epub 2008 Apr 30.
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.
制备并表征了一系列通式为[Au(SR)(P)]和反式-[Pt(SR)₂(P)₂]的金(I)和铂(II)配合物[SR = 2-硫代吡啶(SPy)、2-硫代嘧啶(SPyrim)；P = 1,3,5-三氮杂-7-磷杂金刚烷(PTA)、3,7-二乙酰基-1,3,7-三氮杂-5-磷杂双环[3.3.1]壬烷(DAPTA)]，并评估了它们对一组七种人类癌细胞系的体外细胞毒性。高度水溶性的金(I)配合物[Au(SR)(P)] [P = PTA且SR = SPy (1)、SPyrim (2)；P = DAPTA且SR = SPy (3)、SPyrim (4)]显示出低细胞毒性，而铂(II)配合物反式-[Pt(SR)₂(P)₂] [P = PTA且SR = SPyrim (5)、SPy (6)；P = DAPTA且SR = SPyrim (7)、SPy (8)]与一些已确立的细胞毒性药物的ID₅₀值比较，对卵巢癌、结肠癌、肾癌和黑色素瘤细胞系表现出强效细胞毒性。获得了适合X射线结构表征的2、5、6和8的单晶，研究揭示了5、6和8在固态下的反式构型。
