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Differential Effect...
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Acuña, Ulyana MuñozOhio State University, USA
(author)
Differential Effect of Wortmannolone Derivatives on MDA-MB-231 Breast Cancer Cells.
- Article/chapterEnglish2017
Publisher, publication year, extent ...
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International Institute of Anticancer Research,2017
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Numbers
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LIBRIS-ID:oai:DiVA.org:lnu-101801
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https://urn.kb.se/resolve?urn=urn:nbn:se:lnu:diva-101801URI
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https://doi.org/10.21873/anticanres.11492DOI
Supplementary language notes
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Language:English
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Summary in:English
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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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).
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Added entries (persons, corporate bodies, meetings, titles ...)
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Curley, Robert W,JrOhio State University, USA
(author)
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Fatima, NighatQuaid-i-Azam University, Pakistan;University of Hawaii at Hilo, USA
(author)
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Ahmed, SafiaQuaid-i-Azam University, Pakistan
(author)
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Chang, Leng CheeUniversity of Hawaii at Hilo, USA
(author)
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De Blanco, Esperanza J CarcacheOhio State University, USA
(author)
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Ohio State University, USAQuaid-i-Azam University, Pakistan;University of Hawaii at Hilo, USA
(creator_code:org_t)
Related titles
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In:Anticancer Research: International Institute of Anticancer Research37:4, s. 1617-16230250-70051791-7530
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