Cyclometalated Complexes of Platinum and Palladium with N-(4-Chlorophenyl)--benzoylbenzylideneamine. In Vitro Cytostat

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• 作者：Carmen Navarro-Ranninger ; Isabel Ló ; pez-Solera ; Ví ; ctor M. Gonzá ; lez ; José ; M. Pé ; rez ; Amparo Alvarez-Valdé ; s ; Avelino Martí ; n ; Paul R. Raithby ; José ; R
• 刊名：Inorganic Chemistry
• 出版年：1996
• 出版时间：August 28, 1996
• 年：1996
• 卷：35
• 期：18
• 页码：5181 - 5187
• 全文大小：233K
• 年卷期：v.35,no.18(August 28, 1996)
• ISSN：1520-510X

文摘

In the present paper we report the synthesis and structural IR and¹H and ¹³C NMR characterization offourplatinum(II) and palladium(II) cyclometalated complexes ofthe formula[Pd(4-ClC₆H₄N=C(COC₆H₅)C₆H₄)X]₂,where X = OAc (2) or Cl (3), and[Pt(4-ClC₆H₄N=C(COC₆H₅)C₆H₄)X]₂,where X = Cl (4) or OAc (5).Theacetate-bridged compounds 2 and 5 have anopen-book structure. The chloro-bridged compounds 3 and4 havean unfolded structure. Complex 2 crystallizes in thecentrosymmetric triclinic space group Ps/entities/onemacr.gif">, withZ = 2. Unitcell parameters are as follows: a = 11.765(3) Å,b = 12.862(4) Å, c = 15.022(5) Å,s/gifchars/alpha.gif" BORDER=0> = 84.08(2)s/entities/deg.gif">, s/gifchars/beta2.gif" BORDER=0 ALIGN="middle"> = 78.56(2)s/entities/deg.gif">, s/gifchars/gamma.gif" BORDER=0 > = 83.13(2)s/entities/deg.gif">. All these compounds were screenedagainst MDA-MB 468 (breast carcinoma) and HL-60(leukemic) tumor cells. The low IC₅₀ values ofcompound 5 (1.05 s/entities/mgr.gif">M) and of compound 4 (1.58s/entities/mgr.gif">M) againstMDA-MB 468 and of 0.82 s/entities/mgr.gif">M (5) and 1.37 s/entities/mgr.gif">M (4)against HL-60 relative to cis-DDP (2.67 and 2.07s/entities/mgr.gif">M,respectively) and other cyclometalated compounds suggest that thesynthesized compounds may be regarded ashaving potential antitumor properties. The data suggest that theantiproliferative activity of compound 5 maycorrelate with its covalent binding to DNA and the induction ofimportant modifications on the helix.