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Structure-Activity ...
Structure-Activity Relationship of Niclosamide Derivatives
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- Tang, Zhonghai (författare)
- Ohio State University, USA;Hunan Agricultural University, China
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- Acuña, Ulyana Muñoz (författare)
- Ohio State University, USA
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- Fernandes, Nelson Freitas (författare)
- Ohio State University, USA
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- Chettiar, Somsundaram (författare)
- Ohio State University, USA
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- Li, Pui-Kai (författare)
- Ohio State University, USA
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- De Blanco, Esperanza Carcache (författare)
- Ohio State University, USA
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(creator_code:org_t)
- International Institute of Anticancer Research, 2017
- 2017
- Engelska.
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Ingår i: Anticancer Research. - : International Institute of Anticancer Research. - 0250-7005 .- 1791-7530. ; 37:6, s. 2839-2843
- Relaterad länk:
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https://doi.org/10.2...
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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
Ämnesord
Stäng
- BACKGROUND/AIM: Cancer is a leading cause of death. Hence, this study aimed at the optimization of niclosamide derivatives for the development of new potential anticancer agents.MATERIALS AND METHODS: Niclosamide derivatives were synthesized and tested against a panel of human cancer cells: MDA and MCF7 breast cancer cells, PC3 and DU-145 prostate cancer cells, Hela cervical cancer cells, and HL-60 acute promyelocytic leukemia cells. They were also tested in nuclear factor-ĸappa B (NFĸB), V-Ki-ras2 Kirsten rat sarcoma viral oncogene (KRAS), and mitochondria transmembrane potential (MTP) assays.RESULTS: N-(3,5-Bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide exhibited the most significant cytotoxicity against HL-60 cells, while 5-chloro-N-(2-chlorophenyl)-2-hydroxybenzamide was the most active in the NFĸB assay and 5-chloro-N-(3,5-difluorophenyl)-2-hydroxybenzamide in the MTP assay. 5-chloro-N-(2-chloro-4-(trifluoromethyl) phenyl)-2-hydroxybenzamide and 5-chloro-2-hydroxy-N-(4-hydroxyphenyl)benzamide inhibited both HL-60 cell proliferation and NFĸB.CONCLUSION: In-depth study of the most promising compounds is highly encouraged to further develop into potential anticancer agents those derivatives found to be significantly active.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Cancer och onkologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Cancer and Oncology (hsv//eng)
Nyckelord
- NFĸB
- Niclosamide
- cancer
- cytotoxicity
- mitochondria
- Biokemi
- Biochemistry
- Medicinsk kemi
- Medical Chemistry
- Cell and Organism Biology
- Cell- och organismbiologi
Publikations- och innehållstyp
- ref (ämneskategori)
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