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Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents
In this work, a set of structurally diverse synthetic carbazoles was screened for their anticancer activities. According to structure–activity relationship studies, carbazoles with an N-substituted sulfonyl group exhibited better anticancer activity. Moreover, compound 8h was discovered to show the...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9080423/ https://www.ncbi.nlm.nih.gov/pubmed/35539273 http://dx.doi.org/10.1039/c8ra02939c |
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author | You, Xin Zhu, Daqian Lu, Wenhua Sun, Yichen Qiao, Shuang Luo, Bingling Du, Yongliang Pi, Rongbiao Hu, Yumin Huang, Peng Wen, Shijun |
author_facet | You, Xin Zhu, Daqian Lu, Wenhua Sun, Yichen Qiao, Shuang Luo, Bingling Du, Yongliang Pi, Rongbiao Hu, Yumin Huang, Peng Wen, Shijun |
author_sort | You, Xin |
collection | PubMed |
description | In this work, a set of structurally diverse synthetic carbazoles was screened for their anticancer activities. According to structure–activity relationship studies, carbazoles with an N-substituted sulfonyl group exhibited better anticancer activity. Moreover, compound 8h was discovered to show the most potent anticancer effects on Capan-2 cells by inducing apoptosis and cell cycle arrest in G2/M phase. Finally, the in vivo study demonstrated that 8h prevented the tumor growth in PANC-1 and Capan-2 xenograft models without apparent toxicity. |
format | Online Article Text |
id | pubmed-9080423 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
spelling | pubmed-90804232022-05-09 Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents You, Xin Zhu, Daqian Lu, Wenhua Sun, Yichen Qiao, Shuang Luo, Bingling Du, Yongliang Pi, Rongbiao Hu, Yumin Huang, Peng Wen, Shijun RSC Adv Chemistry In this work, a set of structurally diverse synthetic carbazoles was screened for their anticancer activities. According to structure–activity relationship studies, carbazoles with an N-substituted sulfonyl group exhibited better anticancer activity. Moreover, compound 8h was discovered to show the most potent anticancer effects on Capan-2 cells by inducing apoptosis and cell cycle arrest in G2/M phase. Finally, the in vivo study demonstrated that 8h prevented the tumor growth in PANC-1 and Capan-2 xenograft models without apparent toxicity. The Royal Society of Chemistry 2018-05-10 /pmc/articles/PMC9080423/ /pubmed/35539273 http://dx.doi.org/10.1039/c8ra02939c Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
spellingShingle | Chemistry You, Xin Zhu, Daqian Lu, Wenhua Sun, Yichen Qiao, Shuang Luo, Bingling Du, Yongliang Pi, Rongbiao Hu, Yumin Huang, Peng Wen, Shijun Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents |
title | Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents |
title_full | Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents |
title_fullStr | Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents |
title_full_unstemmed | Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents |
title_short | Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents |
title_sort | design, synthesis and biological evaluation of n-arylsulfonyl carbazoles as novel anticancer agents |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9080423/ https://www.ncbi.nlm.nih.gov/pubmed/35539273 http://dx.doi.org/10.1039/c8ra02939c |
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