17β-雌二醇连接的铂（II）配合物的合成及其对雌激素依赖性和非依赖性乳腺肿瘤细胞的杀伤活性。
Synthesis of 17beta-estradiol-linked platinum(II) complexes and their cytocidal activity on estrogen-dependent and -independent breast tumor cells.
作者信息
Perron Valérie, Rabouin Daniel, Asselin Eric, Parent Sophie, C-Gaudreault René, Bérubé Gervais
机构信息
Département de Chimie-Biologie, Université du Québec à Trois-Rivières, C.P. 500, Trois-Rivières, Québec, Canada, G9A 5H7.
出版信息
Bioorg Chem. 2005 Feb;33(1):1-15. doi: 10.1016/j.bioorg.2004.06.009.
The synthesis of two new highly potent 17beta-estradiol-linked platinum(II) complexes is described. The new molecules are linked at position 16 of the steroid nucleus with an alkyl chain. They are made from estrone in nine chemical steps with an overall yield exceeding 10%. The biological activity of these compounds was evaluated in vitro on estrogen dependent and independent (ER(+) and ER(-)) human breast tumor cell lines: MCF-7 and MDA-MB-231. The novel compounds prove to be highly cytotoxic against breast cancer cell lines. The most cytotoxic derivative shows high affinity for the estrogen receptor alpha.
描述了两种新的高效17β-雌二醇连接的铂（II）配合物的合成。新分子在甾体核的16位通过烷基链连接。它们由雌酮经九个化学步骤制备，总产率超过10%。这些化合物的生物活性在雌激素依赖性和非依赖性（ER(+)和ER(-)）人乳腺肿瘤细胞系：MCF-7和MDA-MB-231上进行了体外评估。新型化合物被证明对乳腺癌细胞系具有高度细胞毒性。细胞毒性最强的衍生物对雌激素受体α具有高亲和力。
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