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新型抗增殖和促凋亡天然醛缩氨基硫脲及其镍(II)和铜(II)配合物的合成、表征与X射线结构

Synthesis, characterization and X-ray structures of new antiproliferative and proapoptotic natural aldehyde thiosemicarbazones and their nickel(II) and copper(II) complexes.

作者信息

Belicchi Ferrari Marisa, Bisceglie Franco, Pelosi Giorgio, Sassi Monica, Tarasconi Pieralberto, Cornia Mara, Capacchi Silvia, Albertini Roberto, Pinelli Silvana

机构信息

Dipartimento di Chimica Generale ed Inorganica, Chimica Analitica, Chimica Fisica, Università di Parma, Parco Area delle Scienze 17/A, I-43100 Parma, Italy.

出版信息

J Inorg Biochem. 2002 Jun 7;90(3-4):113-26. doi: 10.1016/s0162-0134(02)00428-2.

DOI:10.1016/s0162-0134(02)00428-2
PMID:12031803
Abstract

Synthesis and characterization of new thiosemicarbazones derived from natural aldehydes (1-9) have been investigated in order to develop a research program aimed at the development of compounds with antiviral, antibacterial, and antitumor properties. These substances contain both a chain with N and S nucleophilic centers with tuberculostatic activity, and an alkyl or terpenic moiety. In addition, a few nickel(II) and copper(II) complexes (10-18), derived also from the previously studied ligands, were synthesized and characterized by means of NMR and IR techniques. The trans-2-octenal N(1)-phenylthiosemicarbazone and its nickel complex were also characterized by X-ray diffractometry. Biological studies, performed with some of these compounds, have involved both inhibition of cell proliferation and apoptosis tests in vitro on human leukemia cell line U937 to deepen our knowledge on the way these substances interfere with biological processes in leukemic cells.

摘要

为了开展一项旨在开发具有抗病毒、抗菌和抗肿瘤特性化合物的研究计划,对源自天然醛类(1 - 9)的新型硫代氨基脲的合成与表征进行了研究。这些物质既含有具有抑菌活性的含氮和硫亲核中心的链,又含有烷基或萜类部分。此外,还合成了一些同样源自先前研究配体的镍(II)和铜(II)配合物(10 - 18),并通过核磁共振(NMR)和红外(IR)技术对其进行了表征。反式 - 2 - 辛烯醛N(1) - 苯基硫代氨基脲及其镍配合物也通过X射线衍射法进行了表征。使用其中一些化合物进行的生物学研究,包括对人白血病细胞系U937的体外细胞增殖抑制和凋亡试验,以加深我们对这些物质干扰白血病细胞生物学过程方式的了解。

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