Craciunescu G, Scarcia V, Furlani A, Iglesias E P, Ghirvu C, Papaioannou A
Department of Inorganic and Analytical Chemistry, Faculty of Pharmacy, University of Madrid, Spain.
Anticancer Res. 1989 May-Jun;9(3):781-5.
New rhodium(I) complexes, belonging to the general structure [Rh(CO)2(L)], where L were sulfonamide derivatives, were synthesized and characterized by chemical analysis and IR determinations. These complexes were assayed as cytostatic and antitumour agents in vitro against KB cells and in vivo against P388, Ehrich ascites and advanced B16 melanoma. Assays against three Trypanosoma strains were also performed. Among the new compounds, the [Rh(CO)2-(sulfamethoxydiazine)] appeared to be active in all biological systems without showing evident nephrotoxicity. Relationships between biological activity and pi electronic charge localization on N atom of the ligand amidic group were also discussed.
合成了通式为[Rh(CO)2(L)]的新型铑(I)配合物，其中L为磺酰胺衍生物，并通过化学分析和红外光谱测定对其进行了表征。对这些配合物进行了体外抗KB细胞的细胞抑制和抗肿瘤活性测试，以及体内抗P388、艾氏腹水瘤和晚期B16黑色素瘤的活性测试。还对三种锥虫菌株进行了测试。在这些新化合物中，[Rh(CO)2-(磺胺甲氧嗪)]在所有生物系统中均表现出活性，且未显示出明显的肾毒性。还讨论了生物活性与配体酰胺基团中N原子上的π电子电荷定位之间的关系。
