摘要
本文报道非铂族抗肿瘤活性络合物[Sb(Hpdta)]的合成改进和结构测定。结果表明,Sb原子的配位多面体呈畸变缺位五角双锥构型,Sb的一孤对电子处于轴向位置。根据空间构型特征、抗肿瘤活性与Sb—配体螫合强度的关系和胺羧酸的强螫合能力,提出了这一类无机化合物抗肿瘤作用的可能机理。 晶体参数:C_(11)H_(15)N_2O_8Sb,Mr=425.0,正交晶系,空间群Pca2_1,a=8.199(1),b=10.719(1),c=15.247(2)A,V=1340.0A^3,Z=4,D_c=2.107,D_o=2.09gcm^(-3),F(000)=840,μ(MoΚα)=21.1cm^(-1)。1518个可观察衍射参与最小二乘修正,最终偏差因子R=0.032,R_ω(W=σ^(-2))=0.048。
The antamanial chelates of ethylenediaminetetraacetic acid(H4edta), propylenediaminetetraacetic acid (H4pdta)and nitrilotriacetic acid (H3nta) were reported to exhibit inhibitory activities on tumors by Chinese scientists in the end of the fifties. Among these non-platium antitumor agents, [Sb(Hpdta)] was synthesised by a non-cyanic process and characterized by X-ray diffraction analysis.Crystal data:SbC11H15N2O8,Mr= 425. 0,space group Pca21,α= 8. 199( 1) .b= 10. 719(1) ,c = 15. 247 (2) A .V= 1340. 0 A 3,Z = 4,Dc=2.107,D0= 2, 09gcm-3,u(MoKa) = 21. 1cm-1 ,final R = 0. 032,R=0. 048 for 1518 observed data.The geometry of the inner coordination sphere is a distorted ψ-pentagonal bipyramid with a lone electron pair at the axial position, which is similar with that in antimonous diethylenetria-minepentaacetate[Sb(H2etpa)]but different from that in [Sb(Hedta)] by the lone electron pair at the equatorial position. In terms of the feature of the geomatrical configuration,the antitumor activity associated only with moderately stable chelates with antimony,and the strong chelation of complexones, the possible mechanism of antitumor action of the antimonial chelates is proposed.
