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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...

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Detalles Bibliográficos
Autores principales: You, Xin, Zhu, Daqian, Lu, Wenhua, Sun, Yichen, Qiao, Shuang, Luo, Bingling, Du, Yongliang, Pi, Rongbiao, Hu, Yumin, Huang, Peng, Wen, Shijun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2018
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.
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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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