ArticlePloS one2013
Sulphamoylated 2-methoxyestradiol analogues induce apoptosis in adenocarcinoma cell lines.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 28 citations in OpenAlex.
- Radiosensitization of Breast Cancer Cells with a 2-Methoxyestradiol Analogue Affects DNA Damage and Repair Signaling In Vitro.International journal of molecular sciences · 2023Article
- The potential anti-cancer effects of quercetin on blood, prostate and lung cancers: An update.Frontiers in immunology · 2023Review
- In Vitro Effects of Papaverine on Cell Proliferation, Reactive Oxygen Species, and Cell Cycle Progression in Cancer Cells.Molecules (Basel, Switzerland) · 2021Article
- Combination of quercetin and 2-methoxyestradiol inhibits epithelial-mesenchymal transition in PC-3 cell line via Wnt signaling pathway.Future science OA · 2021Article
- Characterization of Signalling Pathways That Link Apoptosis and Autophagy to Cell Death Induced by Estrone Analogues Which Reversibly Depolymerize Microtubules.Molecules (Basel, Switzerland) · 2021Article
- Dysregulation of Catalase by a Sulphamoylated Estradiol Analogue Culminates in Antimitotic Activity and Cell Death Induction in Breast Cancer Cell Lines.Molecules (Basel, Switzerland) · 2021Article
- Sulphamoylated Estradiol Analogue Induces Reactive Oxygen Species Generation to Exert Its Antiproliferative Activity in Breast Cancer Cell Lines.Molecules (Basel, Switzerland) · 2020Article
- Irisin counteracts high glucose and fatty acid-induced cytotoxicity by preserving the AMPK-insulin receptor signaling axis in C2C12 myoblasts.American journal of physiology. Endocrinology and metabolism · 2020Article
- New piperidine derivative DTPEP acts as dual-acting anti-breast cancer agent by targeting ERα and downregulating PI3K/Akt-PKCα leading to caspase-dependent apoptosis.Cell proliferation · 2018Article
- Modes of cell death induced by tetrahydroisoquinoline-based analogs in MDA-MB-231 breast and A549 lung cancer cell lines.Drug design, development and therapy · 2018Article
- The in vitro effects of a novel estradiol analog on cell proliferation and morphology in human epithelial cervical carcinoma.Cellular & molecular biology letters · 2018Article
- A bis-sulphamoylated estradiol derivative induces ROS-dependent cell cycle abnormalities and subsequent apoptosis.PloS one · 2017Article
- In vitro assessment of a computer-designed potential anticancer agent in cervical cancer cells.Biological research · 2016Article
- Cordyceps militaris induces tumor cell death via the caspase‑dependent mitochondrial pathway in HepG2 and MCF‑7 cells.Molecular medicine reports · 2016Article
- Autophagy induced by a sulphamoylated estrone analogue contributes to its cytotoxic effect on breast cancer cells.Cancer cell international · 2016Article
- Effects of 2-methoxyestradiol on apoptosis and HIF-1α and HIF-2α expression in lung cancer cells under normoxia and hypoxia.Oncology reports · 2016Article
- A molecular understanding of D-homoestrone-induced G2/M cell cycle arrest in HeLa human cervical carcinoma cells.Journal of cellular and molecular medicine · 2015Article
- A 2-methoxyestradiol bis-sulphamoylated derivative induces apoptosis in breast cell lines.Cell & bioscience · 2015Article
- Article
- 2-methoxyestradiol and disorders of female reproductive tissues.Hormones & cancer · 2014Review
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
2-Methoxyestradiol (2ME2) is a naturally occurring estradiol metabolite which possesses antiproliferative, antiangiogenic and antitumor properties. However, due to its limited biological accessibility, synthetic analogues have been synthesized and tested in attempt to develop drugs with improved oral bioavailability and efficacy. The aim of this study was to evaluate the antiproliferative effects of three novel in silico-designed sulphamoylated 2ME2 analogues on the HeLa cervical adenocarcinoma cell line and estrogen receptor-negative breast adenocarcinoma MDA-MB-231 cells. A dose-dependent study (0.1-25 μM) was conducted with an exposure time of 24 hours. Results obtained from crystal violet staining indicated that 0.5 μM of all 3 compounds reduced the number of cells to 50%. Lactate dehydrogenase assay was used to assess cytotoxicity, while the mitotracker mitochondrial assay and caspase-6 and -8 activity assays were used to investigate the possible occurrence of apoptosis. Tubulin polymerization assays were conducted to evaluate the influence of these sulphamoylated 2ME2 analogues on tubulin dynamics. Double immunofluorescence microscopy using labeled antibodies specific to tyrosinate and detyrosinated tubulin was conducted to assess the effect of the 2ME2 analogues on tubulin dynamics. An insignificant increase in the level of lactate dehydrogenase release was observed in the compounds-treated cells. These sulphamoylated compounds caused a reduction in mitochondrial membrane potential, cytochrome c release and caspase 3 activation indicating apoptosis induction by means of the intrinsic pathway in HeLa and MDA-MB-231 cells. Microtubule depolymerization was observed after exposure to these three sulphamoylated analogues.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.