We have compared the anti-proliferative activity in vitro, of R₂SnGala (1-3) [R = Me, n-Bu, Ph] and novel R₃SnGala (4, 5) [R = Me, n-Bu] with D-(+)-Galacturonic acid [HGala; Gala^q-, q = (2) and (1) for R₂SnGala and R₃SnGala, respectively] compounds, towards human tumor cell lines of intestinal carcinoma (HCT-116) and breast adenocarcinoma (MCF-7). The new synthesized 4 and 5 compounds were characterized, in solution, by ¹H, ¹³C and ¹¹⁹Sn NMR, that showed that HGala acts as monoanionic moiety and evidenced the dynamic behavior of the compounds, due to inter-conversions involving the anomeric carbon atom of the ligand. Cell viability, apoptosis induction and cell cycle distribution were analyzed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay and flow cytometry, respectively. The cytotoxicity of the compounds, in the micro-submicromolar range, changed in the order of the organotin(IV) moieties, according to 5 > 3 > 2, while 1 and 4, containing Me_nSn(IV) (n = 2,3) moieties, were ineffective. Compound 5 showed peculiar cytotoxic effects. It did not cause time dependent inhibition of cell growth nor accumulated into the cells. Cell death induced by the active 2, 3, and 5, was shown to be apoptotic by measuring the exposure of phosphatidylserine to the outer membrane and the loss of mitochondrial potential. All the cytotoxic compounds induced an accumulation of cells in the subG0/G1phase, while only 2 and 3 perturbed the cell cycle confining viable cells in G0/G1phase. Finally, none of the compounds investigated affected the viability of normal intestinal or liver cells, indicating selectivity towards tumor cells.

我们比较了抗增殖活性在体外，的R ₂ SnGala（1-3）[R = Me中，正丁基，PH]和新颖- [R ₃ SnGala（4，5）[R = Me中的正丁基]用D-（+）-半乳糖醛酸[HGala; 对于肠道癌（HCT-116）和乳腺癌（MCF-7）的人肿瘤细胞系，R ₂ SnGala和R ₃ SnGala的化合物分别分别为Gala ^q-，q =（2）和（1 ）。新合成的4和5种化合物在溶液中的特征在于¹ H，¹³ C和¹¹⁹Sn NMR表明，由于涉及配体的异头碳原子的相互转化，HGala充当单阴离子部分并证明了化合物的动态行为。分别通过3-（4,5-二甲基噻唑-2-基）-2,5-二苯基溴化四氮唑（MTT）比色法和流式细胞仪分析细胞活力，诱导凋亡和细胞周期分布。化合物的细胞毒性在亚微摩尔范围内，按照5  >  3  >  2的顺序依次变化为有机锡（IV）部分，而1和4含Me _n Sn（IV）（n  = 2， 3）部分，无效。化合物5表现出独特的细胞毒性作用。它不会引起时间依赖性的细胞生长抑制，也不会累积到细胞中。细胞死亡诱导活性2，3和5中，示出通过测量磷脂酰丝氨酸的暴露于外膜和线粒体电位的丧失是凋亡。所有的细胞毒性化合物都诱导subG0 / G1期的细胞蓄积，而只有2个和3个扰动了细胞周期，将活细胞限制在G0 / G1期。最后，所研究的化合物均未影响正常肠或肝细胞的活力，表明其对肿瘤细胞的选择性。