Characterization of the Cytotoxic Effect of Naphthalenacetamides Hydrochlorides on Cervical Cancer-Derived Cells.

IF 1.9 4区 医学 Q3 CHEMISTRY, MEDICINAL
Cristina Martinez-Nava, Cuauhtemoc Perez-Gonzalez, Miguel Ángel Zavala-Sanchez, Erick Cuauhtemoc Perez-Montiel, Francisco Javier Lopez-Munoz, Carlos Alberto Mendez-Cuesta
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引用次数: 0

Abstract

Introduction: Cervical cancer is a global health problem due to its high incidence and prevalence in women, mainly in third-world countries. For the treatment of this disease, there are different therapeutic options, but these are not always effective, which gives rise to the search for new compounds using cheminformatics tools.

Objective: The objective of this study was to design, synthesize, and biologically evaluate N-(2- morpholinoethyl)-2-(naphthalen-2-yloxy)acetamide hydrochloride (1) and 2-(naphthalen-2-yloxy)- N-(2-(piperidin-1-yl)ethyl)acetamide hydrochloride (2) on the HeLa cell line in vitro. The referenced cell line from the American Type Culture Collection (ATCC®CCL-2) was used, and the effect on cell viability was determined by MTT metabolic reduction-based assay at 24, 48, and 72 h.

Methods: Therapies directed at the σ1 receptor may be a treatment alternative since this receptor modulates the processes of cell proliferation and angiogenesis, producing cytoprotective or cytotoxic actions depending on the ligand with which it is coupled.

Results: The analysis showed that compounds 1 and 2 presented activity on HeLa cancer cells and viability at micromolar concentrations (1.923 μmol/mL and 0.374 μmol/mL, respectively). Moreover, the effect was maintained for 72 h.

Conclusion: Naphthaleneacetamide derivatives exhibited an inhibitory effect on the HeLa cell line, and the OSIRIS program predicted less toxicity than cisplatin.

盐酸萘乙酰胺对宫颈癌源细胞的细胞毒性作用的表征。
导言:宫颈癌是一个全球性的健康问题,因为它在妇女中发病率和流行率很高,主要是在第三世界国家。对于这种疾病的治疗,有不同的治疗选择,但这些并不总是有效的,这就导致了使用化学信息学工具寻找新的化合物。目的:设计、合成N-(2- morpholinoethyl)-2-(naphthalen-2-yloxy)盐酸乙酰胺(1)和2-(naphthalen-2-yloxy)- N-(2-(pepperidin -1-yl)乙基)盐酸乙酰胺(2),并在体外HeLa细胞系上进行生物学评价。使用来自美国类型培养收集(ATCC®CCL-2™)的参考细胞系,并通过MTT代谢还原法在24、48和72 h时测定对细胞活力的影响。方法:针对σ1受体的治疗可能是一种治疗选择,因为该受体调节细胞增殖和血管生成过程,根据其偶联的配体产生细胞保护或细胞毒性作用。结果:化合物1和2在微摩尔浓度(分别为1.923 μmol/mL和0.374 μmol/mL)下对HeLa癌细胞具有活性和活性。结论:萘乙酰胺衍生物对HeLa细胞系具有抑制作用,且OSIRIS程序预测毒性低于顺铂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Medicinal Chemistry
Medicinal Chemistry 医学-医药化学
CiteScore
4.30
自引率
4.30%
发文量
109
审稿时长
12 months
期刊介绍: Aims & Scope Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.
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