Cytotoxic and proapoptotic effects of new Pd(II) and Pt(II)-complexes with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphosphinin-4-ol-2-oxide.

Polish journal of pharmacology Pub Date : 2004-07-01
Elzbieta Budzisz, Urszula Krajewska, Marek Rózalski
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Abstract

The new palladium (II) and platinum (II) complexes 2 and 3 with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphospinin-4-ol-2-oxide 1 were synthesized and their physicochemical and pharmacological properties were determined. The cytotoxic effects of these complexes were examined on the two human leukemia cell lines, HL-60 and NALM-6. Pd-complex 2 and Pt-complex 3 exerted significant cytotoxic activity. The effects exhibited by these two complexes were comparable to those reported for cis-platin and carboplatin. On the other hand, ligand 1 was not cytotoxic. As determined by caspase-3 activity assay, compounds 2 and 3 differed slightly in their mode of induction of the programmed cell death.

新型Pd(II)和Pt(II)- 3-乙胺酰-2-甲氧基- 2h -1,2-苯并膦-4-醇-2-氧化物配合物的细胞毒性和促凋亡作用。
合成了与3-乙基亚酰基-2-甲氧基- 2h -1,2-苯并草磷蛋白-4-醇-2-氧化物1的新型钯(II)和铂(II)配合物2和3,并测定了它们的理化性质和药理学性质。研究了这些复合物对HL-60和NALM-6两种人白血病细胞系的细胞毒性作用。pd -复合物2和pt -复合物3具有显著的细胞毒活性。这两种复合物的效果与顺铂和卡铂的效果相当。另一方面,配体1没有细胞毒性。通过caspase-3活性测定,化合物2和3诱导程序性细胞死亡的方式略有不同。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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