PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer
As pyrazole and its derivatives have a wide range of biological activities, including anticancer activity, the design of novel pyrazole derivatives has emerged as an important research field. This study describes a novel pyrazole derivative that exerts antitumor and radiosensitizing activities in br...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2022-03-01
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| Series: | Frontiers in Oncology |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/articles/10.3389/fonc.2022.835833/full |
| _version_ | 1819158746513801216 |
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| author | Minsung Kang Navin Pandit Ah-Young Kim Suk Joon Cho Young-Ju Kwon Young-Ju Kwon Jiyeon Ahn Kyu Myung Lee Sangwook Wu Jeong Su Oh Kwan-Young Jung Kwan-Young Jung Jae-Sung Kim Jae-Sung Kim |
| author_facet | Minsung Kang Navin Pandit Ah-Young Kim Suk Joon Cho Young-Ju Kwon Young-Ju Kwon Jiyeon Ahn Kyu Myung Lee Sangwook Wu Jeong Su Oh Kwan-Young Jung Kwan-Young Jung Jae-Sung Kim Jae-Sung Kim |
| author_sort | Minsung Kang |
| collection | DOAJ |
| description | As pyrazole and its derivatives have a wide range of biological activities, including anticancer activity, the design of novel pyrazole derivatives has emerged as an important research field. This study describes a novel pyrazole derivative that exerts antitumor and radiosensitizing activities in breast cancer both in vitro and in vivo. We synthesized a novel pyrazole compound N,N-dimethyl-N’-(3-(1-(4-(trifluoromethyl)phenyl)-1H-pyrazol-4-yl)phenyl)azanesulfonamide (PCW-1001) and showed that it inhibited several oncogenic properties of breast cancer both in vitro and in vivo. PCW-1001 induced apoptosis in several breast cancer cell lines. Transcriptome analysis of PCW-1001-treated cells showed that it regulates genes involved in the DNA damage response, suggesting its potential use in radiotherapy. Indeed, PCW-1001 enhanced the radiation sensitivity of breast cancer cells by modulating the expression of DNA damage response genes. Therefore, our data describe a novel pyrazole compound, PCW-1001, with antitumor and radiosensitizer activities in breast cancer. |
| first_indexed | 2024-12-22T16:29:33Z |
| format | Article |
| id | doaj.art-4db7d44355174c20958e4f145bd37aea |
| institution | Directory Open Access Journal |
| issn | 2234-943X |
| language | English |
| last_indexed | 2024-12-22T16:29:33Z |
| publishDate | 2022-03-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Oncology |
| spelling | doaj.art-4db7d44355174c20958e4f145bd37aea2022-12-21T18:20:05ZengFrontiers Media S.A.Frontiers in Oncology2234-943X2022-03-011210.3389/fonc.2022.835833835833PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast CancerMinsung Kang0Navin Pandit1Ah-Young Kim2Suk Joon Cho3Young-Ju Kwon4Young-Ju Kwon5Jiyeon Ahn6Kyu Myung Lee7Sangwook Wu8Jeong Su Oh9Kwan-Young Jung10Kwan-Young Jung11Jae-Sung Kim12Jae-Sung Kim13Division of Radiation Biomedical Research, Korea Institute of Radiological and Medical Sciences, Seoul, South KoreaDepartment of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon, South KoreaDivision of Radiation Biomedical Research, Korea Institute of Radiological and Medical Sciences, Seoul, South KoreaTherapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon, South KoreaDivision of Radiation Biomedical Research, Korea Institute of Radiological and Medical Sciences, Seoul, South KoreaRadiological and Medico-Oncological Sciences, University of Science and Technology, Seoul, South KoreaDivision of Radiation Biomedical Research, Korea Institute of Radiological and Medical Sciences, Seoul, South KoreaTherapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon, South KoreaResearch & Development (R&D) Center, Pharmcadd, Busan, South KoreaDepartment of Integrative Biotechnology, Sungkyunkwan University, Suwon, South KoreaDepartment of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon, South KoreaTherapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon, South KoreaDivision of Radiation Biomedical Research, Korea Institute of Radiological and Medical Sciences, Seoul, South KoreaRadiological and Medico-Oncological Sciences, University of Science and Technology, Seoul, South KoreaAs pyrazole and its derivatives have a wide range of biological activities, including anticancer activity, the design of novel pyrazole derivatives has emerged as an important research field. This study describes a novel pyrazole derivative that exerts antitumor and radiosensitizing activities in breast cancer both in vitro and in vivo. We synthesized a novel pyrazole compound N,N-dimethyl-N’-(3-(1-(4-(trifluoromethyl)phenyl)-1H-pyrazol-4-yl)phenyl)azanesulfonamide (PCW-1001) and showed that it inhibited several oncogenic properties of breast cancer both in vitro and in vivo. PCW-1001 induced apoptosis in several breast cancer cell lines. Transcriptome analysis of PCW-1001-treated cells showed that it regulates genes involved in the DNA damage response, suggesting its potential use in radiotherapy. Indeed, PCW-1001 enhanced the radiation sensitivity of breast cancer cells by modulating the expression of DNA damage response genes. Therefore, our data describe a novel pyrazole compound, PCW-1001, with antitumor and radiosensitizer activities in breast cancer.https://www.frontiersin.org/articles/10.3389/fonc.2022.835833/fullpyrazole derivativebreast cancerchemotherapyradio-sensitizercombination therapy |
| spellingShingle | Minsung Kang Navin Pandit Ah-Young Kim Suk Joon Cho Young-Ju Kwon Young-Ju Kwon Jiyeon Ahn Kyu Myung Lee Sangwook Wu Jeong Su Oh Kwan-Young Jung Kwan-Young Jung Jae-Sung Kim Jae-Sung Kim PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer Frontiers in Oncology pyrazole derivative breast cancer chemotherapy radio-sensitizer combination therapy |
| title | PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer |
| title_full | PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer |
| title_fullStr | PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer |
| title_full_unstemmed | PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer |
| title_short | PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer |
| title_sort | pcw 1001 a novel pyrazole derivative exerts antitumor and radio sensitizing activities in breast cancer |
| topic | pyrazole derivative breast cancer chemotherapy radio-sensitizer combination therapy |
| url | https://www.frontiersin.org/articles/10.3389/fonc.2022.835833/full |
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