α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer

α-Trifluoromethyl chalcones were prepared and evaluated for their antiproliferative activities against androgen-independent prostate cancer cell lines as well as five additional types of human tumor cell lines. The most potent chalcone 5 showed superior antitumor activity in vivo with both oral and...

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Detalles Bibliográficos
Autores principales: Saito, Yohei, Mizokami, Atsushi, Izumi, Kouji, Naito, Renato, Goto, Masuo, Nakagawa-Goto, Kyoko
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8126091/
https://www.ncbi.nlm.nih.gov/pubmed/34068627
http://dx.doi.org/10.3390/molecules26092812
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author Saito, Yohei
Mizokami, Atsushi
Izumi, Kouji
Naito, Renato
Goto, Masuo
Nakagawa-Goto, Kyoko
author_facet Saito, Yohei
Mizokami, Atsushi
Izumi, Kouji
Naito, Renato
Goto, Masuo
Nakagawa-Goto, Kyoko
author_sort Saito, Yohei
collection PubMed
description α-Trifluoromethyl chalcones were prepared and evaluated for their antiproliferative activities against androgen-independent prostate cancer cell lines as well as five additional types of human tumor cell lines. The most potent chalcone 5 showed superior antitumor activity in vivo with both oral and intraperitoneal administration at 3 mg/kg. Cell-based mechanism of action studies demonstrated that 5 induced cell accumulation at sub-G1 and G2/M phases without interfering with microtubule polymerization. Furthermore, several cancer cell growth-related proteins were identified by using chalcone 5 as a bait for the affinity purification of binding proteins.
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spelling pubmed-81260912021-05-17 α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer Saito, Yohei Mizokami, Atsushi Izumi, Kouji Naito, Renato Goto, Masuo Nakagawa-Goto, Kyoko Molecules Article α-Trifluoromethyl chalcones were prepared and evaluated for their antiproliferative activities against androgen-independent prostate cancer cell lines as well as five additional types of human tumor cell lines. The most potent chalcone 5 showed superior antitumor activity in vivo with both oral and intraperitoneal administration at 3 mg/kg. Cell-based mechanism of action studies demonstrated that 5 induced cell accumulation at sub-G1 and G2/M phases without interfering with microtubule polymerization. Furthermore, several cancer cell growth-related proteins were identified by using chalcone 5 as a bait for the affinity purification of binding proteins. MDPI 2021-05-10 /pmc/articles/PMC8126091/ /pubmed/34068627 http://dx.doi.org/10.3390/molecules26092812 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Saito, Yohei
Mizokami, Atsushi
Izumi, Kouji
Naito, Renato
Goto, Masuo
Nakagawa-Goto, Kyoko
α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer
title α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer
title_full α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer
title_fullStr α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer
title_full_unstemmed α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer
title_short α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer
title_sort α-trifluoromethyl chalcones as potent anticancer agents for androgen receptor-independent prostate cancer
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8126091/
https://www.ncbi.nlm.nih.gov/pubmed/34068627
http://dx.doi.org/10.3390/molecules26092812
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