Synthesis and X-ray structure analysis of cytotoxic heptacoordinated Salan hafnium(IV) complexes stabilized with 2,6-dipicolinic acid

被引：7

作者：

Zhao, Tiankun ^{[1
]}

Wang, Peng ^{[1
]}

Liu, Nan ^{[1
]}

Zhao, Wenzhuo ^{[1
]}

Yang, Mingjun ^{[1
]}

Li, Shanjia ^{[1
]}

Yang, Zhongduo ^{[1
]}

Sun, Bolu ^{[1
]}

Huhn, Thomas ^{[2
,3
]}

机构：

[1] Lanzhou Univ Technol, Coll Life Sci & Engn, Lanzhou 730050, Peoples R China

[2] Univ Konstanz, Fachbereich Chem, Univ Str 10, D-78457 Constance, Germany

[3] Univ Konstanz, Konstanz Res Sch Chem Biol, Univ Str 10, D-78457 Constance, Germany

来源：

JOURNAL OF INORGANIC BIOCHEMISTRY | 2023年 / 240卷

关键词：

Hafnium complexes; Anti-tumoral activity; Aqueous stability; Cellular uptake; Apoptosis; 6-dipicolinic acid; TITANIUM(IV) COMPLEXES; ZIRCONIUM; POLYMERIZATION; NANOPARTICLES; METALLOCENE; TITANOCENE; EFFICACY; LIGANDS; TUMOR;

D O I：

10.1016/j.jinorgbio.2022.112094

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Four novel Salan Hf(IV) complexes stabilized by 2,6-dipicolinic acid (Dipic) were synthesized and characterized by 1H, 13C NMR and X-ray diffraction spectroscopy. These Hf(IV) bis-chelates could be obtained in good to excellent yields (88%-91%) and demonstrated rather good stability in aqueous media and on silica gel. [L2Hf(IV)Dipic4-H,Cl] containing steric bulk L2 were stable in about 10% H2O (H2O/THF (v/v)), however, [L1Hf(IV)Dipic4-H,Cl] with non-steric L1 could slowly dissociate and release nontoxic L1. [L1-2Hf(IV)Dipic4-Cl] showed excellent anti-tumoral activity in the range of cisplatin (Hela S3: IC50 = 3.5 +/- 0.4 mu M, Hep G2: IC50 = 11.2 +/- 2.1 mu M). In addition, the cellular uptake and apoptosis investigation of [L1Hf(IV)Dipic4-Cl] suggested a fast cellular uptake process against Hela S3 cells with an almost exclusive induced apoptosis cell death path.

引用

页数：7

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