New Di(heteroaryl)ethenes as Apoptotic Anti-proliferative Agents Towards Breast Cancer: Design, One-Pot Synthesis and In Vitro Evaluation

被引：6

作者：

Bonaccorso, Carmela ^{[1
]}

Naletova, Irina ^{[2
]}

Satriano, Cristina ^{[2
,3
]}

Spampinato, Giorgia ^{[4
,5
]}

Barresi, Vincenza ^{[4
,5
]}

Fortuna, Cosimo G. ^{[1
]}

机构：

[1] Univ Catania, Dipartimento Sci Chim, Lab Modellist Mol & Composti Eterocicl ModHet, Viale A Doria 6, I-95125 Catania, Italy

[2] CIRCMSB, Via Celso Ulpiani 27, I-70126 Bari, Italy

[3] Univ Catania, Dipartimento Sci Chim, Lab NanobioInterfacce Ibride NHIL, Viale A Doria 6, I-95125 Catania, Italy

[4] Univ Catania, BRIT, I-95125 Catania, Italy

[5] Univ Catania, Dipartimento Sci Biomed & Biotecnol, Sez Biochim Med, Via S Sofia 64, I-95125 Catania, Italy

来源：

CHEMISTRYSELECT | 2020年 / 5卷 / 08期

关键词：

Cancer; Cytotoxicity; Di(heteroaryl)ethenes; Drug design; Subcellular localization; MULTIDRUG-RESISTANCE; STRATEGIES; MITOCHONDRIA; CHEMOTHERAPY; MECHANISMS; CATIONS; DRUGS; DNA;

D O I：

10.1002/slct.201903502

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A new series of di(heteroaryl)ethenes was designed and synthesized by combining 5-(dichlorophenyl)-furan-2-yl and N-substituted pyridinum moieties. All the synthesized compounds were screened for their anticancer activity against the MCF-7 human breast cancer cell line. Most of the tested compounds showed moderate to potent cell growth inhibition; in particular, four of these exhibited promising cytotoxicity against this cell line, with IC50 values in the range of 0.30-0.005 mu M. In addition, the potential mechanism of cell growth inhibition and apoptotic induction by these compounds was investigated by using flow cytometry and confocal microscopy. Based on these results, we identified a new and alternative class of anticancer agents that have the potential to be developed as leads.

引用

页码：2581 / 2587

页数：7

共 42 条

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