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通过催化不对称氢膦化反应合成手性膦-N-杂环卡宾铂配合物及其对 MKN74 和 MCF7 癌细胞系的细胞毒性。

Chelating Phosphine-N-Heterocyclic Carbene Platinum Complexes via Catalytic Asymmetric Hydrophosphination and Their Cytotoxicity Toward MKN74 and MCF7 Cancer Cell Lines.

机构信息

Division of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore 637371, Singapore.

Lee Kong Chian School of Medicine, Nanyang Technological University Singapore, 11 Mandalay Road, Singapore 308232, Singapore.

出版信息

Inorg Chem. 2021 Nov 15;60(22):17276-17287. doi: 10.1021/acs.inorgchem.1c02625. Epub 2021 Oct 28.

DOI:10.1021/acs.inorgchem.1c02625
PMID:34709031
Abstract

A series of activated vinyl azoles was hydrophosphinated in the presence of a chiral palladacycle catalyst under mild conditions to give enantioenriched phosphine azoles with moderate enantioselectivities and yields. The racemic phosphine azoles were transformed into eleven novel chelating phosphine-N-heterocyclic carbene (NHC) platinum complexes. The drug efficacies of nine selected phosphine-NHC platinum(II) chlorides in two cancer cell lines (MKN74 and MCF7) were evaluated, and two were found to exhibit activities comparable to that of cisplatin.

摘要

在温和条件下,一系列活化的乙烯基唑在手性钯环催化剂的存在下进行氢膦化反应,得到具有中等对映选择性和收率的手性膦唑。外消旋膦唑被转化为十一种新型螯合膦-N-杂环卡宾(NHC)铂配合物。评估了九种选定的膦-NHC 铂(II)氯化物在两种癌细胞系(MKN74 和 MCF7)中的药效,其中两种表现出与顺铂相当的活性。

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