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New Pt(II) complexes with 3 ’ -methyl tetrahydro-4 H -thiopyranspiro-5 ’ -hydantoin: synthesis, theoretical and cytotoxic investigation
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-09-30 , DOI: 10.1007/s00044-020-02639-9
Adriana Georgieva Bakalova , Rossen Todorov Buyukliev , Emilyia Demireva Cherneva

Three new platinum complexes with chemical formulas cis-[PtL2Cl2], cis-[PtL2I2] and cis-[PtL(NH3)Cl2], where L is 3-methyl-4-thio-1H-tetrahydropyranspiro-5-hydantoin were synthesized and studied. The spectral and theoretical investigations proved that ligand coordinates through sulfur atom from tetrahydrothiopyrane fragment by monodentate manner with platinum ion. The newly synthesized compounds were tested for cytotoxic activity in vitro against four human tumor cell lines using MTT dye-reduction assay for cell viability. The tested compounds displayed cytotoxic effects in a concentration-dependent manner. Complex 2 as well as complex 3 have similar cytotoxicity to that of the prototype drug cisplatin on colon adenocarcinoma model HT-29.



中文翻译:

具有3'-甲基四氢-4 H-硫代吡喃螺-5'-乙内酰脲的新型Pt(II)配合物:合成,理论和细胞毒性研究

三个新的铂络合物与化学式顺式- [专利文献22 ],顺式- [专利文献22 ]和- [PTL(NH 3)氯2 ],其中大号是3 ' -甲基-4-硫基-1- ħ -tetrahydropyranspiro-5 '-乙内酰脲的合成和研究。光谱和理论研究证明,配体通过四齿硫吡喃片段中的硫原子与铂离子单齿配位。使用MTT染料还原法检测新合成的化合物对四种人类肿瘤细胞系的体外细胞毒性活性,以检测细胞活力。被测化合物以浓度依赖性的方式显示出细胞毒性作用。复合物2和复合物3对结肠腺癌模型HT-29具有与原型药物顺铂相似的细胞毒性。

更新日期:2020-10-07
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