Wesselinova Diana, Neykov Mihail, Kaloyanov Nikolay, Toshkova Reneta, Dimitrov Georgi
Institute of Experimental Pathology and Parasitology, Bulgarian Academy of Sciences, Acad. G. Bonchev Street, Bl. 25, 1113 Sofia, Bulgaria.
Eur J Med Chem. 2009 Jun;44(6):2720-3. doi: 10.1016/j.ejmech.2009.01.036. Epub 2009 Feb 10.
Synthesis and impact on the tumour growth of palladium(II) complex of 5-amino-1,10-phenanthroline Pd(5-NH(2)-phen)(2)(NO(3))(2) and the protonated dimer (phen)(2)(H(+))(BF(4)(-)) have been described. In the reported experiments a cancerous (100% lethality) myeloid subcutaneous tumour (with Graffi-tumour origin) in hamsters was used. The animals were injected i.p. with different doses of the substances. The longest mean survival time (1.65 times longer than the controls) was achieved when the substance Pd(5-NH(2)-phen)(2)(NO(3))(2) was injected into the animals. One of the animals even survived until the 71st day, which is 2.2 times longer than the controls. The compound (phen)(2)(H(+))(BF(4)(-)) prolonged the mean life-time of the animals 1.4 times in comparison to the controls. On the other hand, the Pd(II) complex of 1,10-phenanthroline, Pd(phen)(2)(H(2)O)(NO(3))(2), did not reveal any antitumour activity. Our experience concerning the effect of other drugs on this tumour has shown a survival time no longer than 4-5d after the death of the controls.
已描述了5-氨基-1,10-菲咯啉钯（II）配合物Pd(5-NH(2)-phen)(2)(NO(3))(2)以及质子化二聚体(phen)(2)(H(+))(BF(4)(-))的合成及其对肿瘤生长的影响。在报道的实验中，使用了仓鼠的一种癌性（100%致死率）髓样皮下肿瘤（起源于格拉夫氏肿瘤）。给动物腹腔注射不同剂量的这些物质。当向动物注射物质Pd(5-NH(2)-phen)(2)(NO(3))(2)时，实现了最长的平均存活时间（比对照组长1.65倍）。其中一只动物甚至存活到了第71天，这比对照组长2.2倍。化合物(phen)(2)(H(+))(BF(4)(-))使动物的平均寿命比对照组延长了1.4倍。另一方面，1,10-菲咯啉的钯（II）配合物Pd(phen)(2)(H(2)O)(NO(3))(2)未显示出任何抗肿瘤活性。我们关于其他药物对这种肿瘤影响的经验表明，在对照组死亡后存活时间不超过4 - 5天。
