Abstract The Cu(I) alkyne azide click reaction of 17α-ethynylestradiol and di-tert-butyl (2-azidopropane-1,3-diyl)dicarbamate afforded the novel 1,4 disubstituted 1,2,3 triazole and estrogen-based ligand 2-(4-(estradiol)-1H-1,2,3-triazol-1-yl)propane-1,3-diamine, EDiolDap. Reaction of EDiolDap with Pt(II) DMSO precursors, cis-[PtCl2(DMSO)2] and cis-[Pt(CBDCA)(DMSO)2] gave the corresponding Pt(II) estrogen linked complexes [PtCl2(EDiolDap)] and [Pt(CBDCA)(EDiolDap)] respectively in good yield. Both Pt(II) estrogen linked complexes exhibited superior activity as compared to cisplatin and carboplatin in 2D culture and exhibited ca. 30 fold higher activity, in terms of IC50 values, against ER+ cancer cells (cervical, breast and ovarian) as compared to the reference ER− colon cancer line. [PtCl2(EDiolDap)] and [Pt(CBDCA)(EDiolDap)] retained their anti-tumour activity in an ovarian 3D spheroid culture model and reduced the viability of ovarian cancer cell spheroids ca. 9-fold and 5-fold better, respectively, as compared to cisplatin.

中文翻译：

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新型Pt（II）雌激素连接复合物的合成，表征和体外抗肿瘤潜力

摘要17α-乙炔基雌二醇与2-（2-叠氮基丙烷-1,3-二基）二氨基甲酸二叔丁酯的Cu（I）炔叠氮化物点击反应提供了新型的1,4二取代的1,2,3三唑和雌激素基配体2-（4-（雌二醇）-1H-1,2,3-三唑-1-基）丙烷-1,3-二胺，EDiolDap。EDiolDap与Pt（II）DMSO前体，顺式[[PtCl2（DMSO）2]和顺式[Pt（CBDCA）（DMSO）2]的反应产生相应的Pt（II）雌激素连接复合物[PtCl2（EDiolDap）]和[Pt（CBDCA）（EDiolDap）]分别具有良好的收率。与顺铂和卡铂在2D培养中相比，Pt（II）雌激素连接的复合物均显示出更高的活性，并且显示出约。与参考ER-结肠癌细胞系相比，就IC50值而言，针对ER +癌细胞（子宫颈，乳腺癌和卵巢癌）的活性提高了30倍。[PtCl2（EDiolDap）]和[Pt（CBDCA）（EDiolDap）]在卵巢3D球体培养模型中保留了其抗肿瘤活性，并降低了卵巢癌细胞球体的生存能力。与顺铂相比，分别提高了9倍和5倍。