ArticlePloS one2012
In vitro evaluation of ESE-15-ol, an estradiol analogue with nanomolar antimitotic and carbonic anhydrase inhibitory activity.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 30 citations in OpenAlex.
- Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy.Signal transduction and targeted therapy · 2023Review
- Cellular, Biophysical and in Silico Binding Study of β-Estradiol-6-one 6- (O-carboxy methyl Oxime) with Tubulin in Search of Antimitotic Derivative of 2-Methoxy Estradiol.Cell biochemistry and biophysics · 2023Article
- The emerging role of BET inhibitors in breast cancer.Breast (Edinburgh, Scotland) · 2020Review
- Novel sulphamoylated 2-methoxy estradiol derivatives inhibit breast cancer migration by disrupting microtubule turnover and organization.Cancer cell international · 2019Article
- A Combination of an Antimitotic and a Bromodomain 4 Inhibitor Synergistically Inhibits the Metastatic MDA-MB-231 Breast Cancer Cell Line.BioMed research international · 2019Article
- Exposure of Breast and Lung Cancer Cells to a Novel Estrone Analog Prior to Radiation Enhances Bcl-2-Mediated Cell Death.International journal of molecular sciences · 2018Article
- A novel non-sulphamoylated 2-methoxyestradiol derivative causes detachment of breast cancer cells by rapid disassembly of focal adhesions.Cancer cell international · 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
- In vitro assessment of a computer-designed potential anticancer agent in cervical cancer cells.Biological research · 2016Article
- Autophagy induced by a sulphamoylated estrone analogue contributes to its cytotoxic effect on breast cancer cells.Cancer cell international · 2016Article
- Carbonic anhydrase 1 is a promising biomarker for early detection of non-small cell lung cancer.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2016Article
- Antimitotic drugs in the treatment of cancer.Cancer chemotherapy and pharmacology · 2015Review
- Advances in Anti-Cancer Drug Development Targeting Carbonic Anhydrase IX and XII.Topics in anti-cancer research · 2015Article
- Probing the surface of human carbonic anhydrase for clues towards the design of isoform specific inhibitors.BioMed research international · 2015Review
- A 2-methoxyestradiol bis-sulphamoylated derivative induces apoptosis in breast cell lines.Cell & bioscience · 2015Article
- Ex vivo apoptotic and autophagic influence of an estradiol analogue on platelets.Experimental hematology & oncology · 2015Article
- Ultrastructural changes of erythrocytes in whole blood after exposure to prospective in silico-designed anticancer agents: a qualitative case study.Biological research · 2014Article
- Novel estradiol analogue induces apoptosis and autophagy in esophageal carcinoma cells.Cellular & molecular biology letters · 2014Article
- An estrogen analogue and promising anticancer agent refrains from inducing morphological damage and reactive oxygen species generation in erythrocytes, fibrin and platelets: a pilot study.Cancer cell international · 2014Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Antimitotic compounds are still one of the most widely used chemotherapeutic anticancer drugs in the clinic today. Given their effectiveness against cancer it is beneficial to continue enhancing these drugs. One way is to improve the bioavailability and efficacy by synthesizing derivatives that reversibly bind to carbonic anhydrase II (CAII) in red blood cells followed by a slow release into the blood circulation system. In the present study we describe the in vitro biological activity of a reduced derivative of 2-ethyl-3-O-sulphamoyl-estradiol (2EE), 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10),15-tetraen-17-ol (ESE-15-ol). ESE-15-ol is capable of inhibiting carbonic anhydrase activity in the nanomolar range and is selective towards a mimic of carbonic anhydrase IX when compared to the CAII isoform. Docking studies using Autodock Vina suggest that the dehydration of the D-ring plays a role towards the selectivity of ESE-15-ol to CAIX and that the binding mode of ESE-15-ol is substantially different when compared to 2EE. ESE-15-ol is able to reduce cell growth to 50% after 48 h at 50-75 nM in MCF-7, MDA-MB-231, and MCF-12A cells. The compound is the least potent against the non-tumorigenic MCF-12A cells. In vitro mechanistic studies demonstrate that the newly synthesized compound induces mitochondrial membrane depolarization, abrogates the phosphorylation status of Bcl-2 and affects gene expression of genes associated with cell death and mitosis.
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