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新型对映体纯的吡唑啉酮-钌配合物的抗肿瘤活性

Antitumor activity of new enantiopure pybox-ruthenium complexes.

作者信息

Menéndez-Pedregal Estefania, Díez Josefina, Manteca Ángel, Sánchez Jesús, Bento Ana C, García-Navas Rósula, Mollinedo Faustino, Gamasa M Pilar, Lastra Elena

机构信息

Departamento de Química Orgánica e Inorgánica, Instituto de Química Organometálica "Enrique Moles" (Unidad Asociada al C.S.I.C.). Universidad de Oviedo, 33006 Oviedo, Principado de Asturias, Spain.

出版信息

Dalton Trans. 2013 Oct 14;42(38):13955-67. doi: 10.1039/c3dt51160j. Epub 2013 Aug 8.

Abstract

New ruthenium complexes containing enantiopure 2,6-bis[4'(R)-phenyloxazolin-2'-il-pyridine] ((R,R)-Ph-pybox), 2,6-bis[4'(S)-isopropyloxazolin-2'-il-pyridine] ((S,S)-(i)Pr-pybox) or 2,6-bis[4'(R)-isopropyloxazolin-2'-il-pyridine] ((R,R)-(i)Pr-pybox) and water soluble 1,3,5-triaza-7-phosphaadamantane (PTA) or N-substituted PTA phosphanes have been synthesized in high yields and fully characterized. The interactions of these compounds with plasmidic DNA and their cytotoxic activity against the human cervical cancer HeLa cell line are reported, pointing out for the first time the different behaviour of ruthenium enantiomers affecting the cell cycle in HeLa tumor cells.

摘要

已高产率合成并充分表征了含有对映体纯的2,6 - 双[4'(R)-苯基恶唑啉-2'-基吡啶]((R,R)-Ph-pybox)、2,6 - 双[4'(S)-异丙基恶唑啉-2'-基吡啶]((S,S)-(i)Pr-pybox)或2,6 - 双[4'(R)-异丙基恶唑啉-2'-基吡啶]((R,R)-(i)Pr-pybox)以及水溶性1,3,5 - 三氮杂 - 7 - 磷杂金刚烷(PTA)或N - 取代PTA膦的新型钌配合物。报道了这些化合物与质粒DNA的相互作用及其对人宫颈癌HeLa细胞系的细胞毒性活性,首次指出钌对映体在HeLa肿瘤细胞中影响细胞周期的不同行为。

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