PHOSPHINEGOLD(I) COMPLEXES CONTAINING THE PURINE-6-THIOLATE ANION, AND THEIR ANTIARTHRITIC ACTIVITY

A series of complexes of the general formulae R3PAu(6-mp), R3P = Et3P, Ph3P, Cy3P, PhMe2P, (o-tol)3P, (m-tol)3P or (p-tol)3P, (AuCl)Ph2P(CH2)nPPh2(Au(6-mp)), n = 2 or 3, and Ph2P(CH2)nPPh2(Au(6-mp))2, n = 1, 2 or 3 and 6-mp is the anion derived from 6-mercaptopurine (purine-6-thiol), have been prepared and characterized by spectroscopic methods (i.r., H-1, C-13, P-31 n.m.r. and f.a.b. m.s.) and, in the case of the Ph3PAu(6-mp) complex, by single-crystal X-ray diffraction methods. The spectroscopic data show that the 6-mp ligand coordinates as a thiolate ligand and that the gold atoms exist in linear P-Au-S (or P-Au-Cl) geometries. This has been confirmed by an X-ray study on Ph3PAu(6-mp), isolated as an ethanol solvate; the study shows the gold atom to be linearly coordinated by the phosphorus and sulfur atoms: Au-P(1) 2.237(2), Au-S(6) 2.287(1) angstrom and P-Au-S 173-71(6)-degrees. Crystals of Ph3PAu(6-mp).EtOH are triclinic, space group P1BAR, with unit cell dimensions a 11 .066(3), b 13.552(3), c 8.705(2) angstrom, alpha 91.51(2), beta 113.06(2), gamma 89.69(2)-degrees, V 1200.8(5) angstrom3, Z 2. The structure was; refined by a full-matrix least-squares procedure to R 0.034 for 3978 reflections with 1 greater-than-or-equal-to 3.0sigma(I). Preliminary results of testing for antiarthritic activity among the new complexes in rats are also reported showing that some of them are more potent/less toxic than current gold(i) thiolates used clinically.