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Title: (. mu. -1,1 prime -Bis(diphenylphosphine)ferrocene)bis(chlorogold): Synthesis, iron-57 and gold-197 Moessbauer spectroscopy, x-ray crystal structure, and antitumor activity

Journal Article · · Inorganic Chemistry; (USA)
DOI:https://doi.org/10.1021/ic00317a027· OSTI ID:7108010
; ; ; ;  [1]; ; ;  [2]
  1. Smith Kline and French Labs., King of Prussia, PA (USA)
  2. Northeastern Univ., Boston, MA (USA)

The title compound 2, Fdpp(AuCl){sub 2}, synthesized via the addition of Fdpp (1) to an aqueous solution of ((HOCH{sub 2}CH{sub 2}){sub 2}S)AuCl generated in situ by the thiodiglycol reduction of HAuCl{sub 4} showed a {sup 31}P({sup 1}H) NMR chemical shift at {delta} 27.39, which was downfield from that of 1 at {delta} -17.34 relative to (CH{sub 3}O)PO. The {sup 57}Fe Moessbauer spectrum of 2 is a doublet with parameters (IS = 0.50 mm/s relative to Fe, QS = 2.33 mm/s) similar to those of ferrocene. The {sup 197}Au Moessbauer spectrum of 2 is an asymmetric doublet (QS = 6.93 mm/s) with an IS of 3.81 mm/s relative to Au metal. Fdpp(AuCl){sub 2} crystallized in space group P{bar 1} with lattice constants a = 16.192 (4) {angstrom}, b = 16.921 (4) {angstrom}, and c = 10.878 (5) {angstrom} with Z = 3. Two crystallographically independent molecules, A and B, were observed in the structure of 2 with a chloroform solvate molecule per 1.5 formula units of the gold complex. For A, the P atoms are 180{degree} opposed and the rings exactly staggered, while in B the P atoms are 150{degree} apart and the rings are partially staggered. The P-Au-Cl linkage is nearly linear, and the bond distances fall within normal ranges. Evaluation in an ip P388 leukemia mouse model showed 1 and 2 to have only marginal activity with an increased life span (ILS) relative to untreated controls of 30% at a maximally tolerated dose (MTD) of 231 {mu}mol/kg and 40% ILS at 4 {mu}mol/kg, respectively. 27 refs., 4 figs., 3 tabs.

OSTI ID:
7108010
Journal Information:
Inorganic Chemistry; (USA), Vol. 28:18; ISSN 0020-1669
Country of Publication:
United States
Language:
English