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Synthetic Naphthoquinone Derivatives as Anticancer Agents in Ovarian Cancer: Cytotoxicity Assay and Investigation of Possible Biological Mechanisms Action
Chemistry & Biodiversity ( IF 2.9 ) Pub Date : 2022-10-27 , DOI: 10.1002/cbdv.202200807
Renata Dalmaschio Daltoé 1 , Leticia Batista Azevedo Rangel 1 , Maicon Delarmelina 2 , Klesia Pirola Madeira 3 , Marcella Leite Porto 4 , Silvana Santos Meirelles 5 , Isabella Dos Santos Guimarães 6 , Éclair Venturini Filho 7 , Alan Reinke Pereira 7 , Rafael de Queiroz Ferreira 7 , Gabriel Fernandes Souza Dos Santos 7 , Izabela de França Schaffel 7 , José Walkimar de Mesquita Carneiro 8 , Artur M S Silva 9 , Sandro José Greco 7
Affiliation  

In this study, eight naphthoquinone derivatives were synthesized in yields ranging from 52 to 96% using easy, fast, and low-cost methodologies. All naphthoquinone derivatives were screened for their in vitro anti-proliferative activities against OVCA A2780 cancer cell lines. Amongst all analysed compounds, derivatives 35 presented the most prominent cytotoxic potential. Naphthoquinones 3 and 4, bearing sulfur-containing groups, were identified as having high potential for ROS production, in particular the superoxide anion. Furthermore, 3 and 4 compounds caused a decrease in the cell population in G0/G1 and induced more than 90% of the cell population to apoptosis. Compound 5 did not act in any of these processes. Finally, compounds 35 were tested for their inhibitory ability against PI3K and MAPK. Compounds 3 and 4 do not inhibit the PI3K enzyme. On the other hand, the naphthoquinone-polyphenol 5 was only able to inhibit the percentage of cells expressing pERK.

中文翻译:

合成萘醌衍生物作为卵巢癌抗癌剂:细胞毒性测定和可能的生物学作用机制研究

在这项研究中,使用简单、快速和低成本的方法合成了八种萘醌衍生物,产率在 52% 到 96% 之间。筛选了所有萘醌衍生物对 OVCA A2780 癌细胞系的体外抗增殖活性。在所有分析的化合物中,衍生物35具有最突出的细胞毒性潜力。带有含硫基团的萘醌34被确定为具有产生 ROS 的高潜力,特别是超氧阴离子。此外,34化合物导致 G0/G1 期细胞群减少,并诱导超过 90% 的细胞群发生凋亡。化合物5在这些过程中没有任何作用。最后,测试了化合物35对 PI3K 和 MAPK 的抑制能力。化合物34不抑制 PI3K 酶。另一方面,萘醌-多酚5只能抑制表达 pERK 的细胞百分比。
更新日期:2022-10-27
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