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Differential Effect...
Differential Effect of Wortmannolone Derivatives on MDA-MB-231 Breast Cancer Cells.
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- Acuña, Ulyana Muñoz (author)
- Ohio State University, USA
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- Curley, Robert W, Jr (author)
- Ohio State University, USA
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- Fatima, Nighat (author)
- Quaid-i-Azam University, Pakistan;University of Hawaii at Hilo, USA
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- Ahmed, Safia (author)
- Quaid-i-Azam University, Pakistan
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- Chang, Leng Chee (author)
- University of Hawaii at Hilo, USA
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- De Blanco, Esperanza J Carcache (author)
- Ohio State University, USA
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(creator_code:org_t)
- International Institute of Anticancer Research, 2017
- 2017
- English.
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In: Anticancer Research. - : International Institute of Anticancer Research. - 0250-7005 .- 1791-7530. ; 37:4, s. 1617-1623
- Related links:
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http://ar.iiarjourna...
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https://urn.kb.se/re...
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https://doi.org/10.2...
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Abstract
Subject headings
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- BACKGROUND/AIM: The survival rate of women diagnosed with triple-negative breast-cancer (TNBC) remains low. Hence, this study aimed at the chemical and biological optimization of furanosteroid derivatives for the treatment of this type of malignancy using TNBC cells.MATERIALS AND METHODS: Semi-synthetic analogs of wortmannolone (1-6) that negatively affected the aberrant pathways in tumor cells were evaluated in hormone-independent breast cancer cells using western blot and cell-cycle analysis.RESULTS: Wortmannolone derivatization generated NF-ĸB inhibitors as new lead structures for further development. Compound (3) was found to be the most significantly active lead.CONCLUSION: Structure-activity analysis in the present study showed that acetylation of the hydroxyl groups and substitution on C3 and C17 of wortmannolone enhanced biological activity. Alpha-substitution of the acetyl group in C3 on ring A (compound 3) resulted in ROS inducing effect; however, presence of an acetyl group in β-position of C3 displayed the highest NF-ĸB p65 inhibitory activity (0.60 μM).
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Keyword
- Furanosteroids
- K-Ras
- NF-ĸB p65
- ROS
- breast cancer cells
- wortmannolone
- Biochemistry
- Biokemi
Publication and Content Type
- ref (subject category)
- art (subject category)
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