Design, synthesis and biological evaluation of: N -arylsulfonyl carbazoles as novel anticancer agents

Xin You; Daqian Zhu; Wenhua Lu; Yichen Sun; Shuang Qiao; Bingling Luo; Yongliang Du; Rongbiao Pi; Yumin Hu; Peng Huang; Shijun Wen

doi:10.1039/c8ra02939c

Design, synthesis and biological evaluation of: N -arylsulfonyl carbazoles as novel anticancer agents

Xin You, Daqian Zhu, Wenhua Lu, Yichen Sun, Shuang Qiao, Bingling Luo, Yongliang Du, Rongbiao Pi, Yumin Hu, Peng Huang, Shijun Wen

Translational Molecular Pathology

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	17183-17190
Number of pages	8
Journal	RSC Advances
Volume	8
Issue number	31
DOIs	https://doi.org/10.1039/c8ra02939c
State	Published - 2018

ASJC Scopus subject areas

General Chemistry
General Chemical Engineering

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abstract = "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.",

author = "Xin You and Daqian Zhu and Wenhua Lu and Yichen Sun and Shuang Qiao and Bingling Luo and Yongliang Du and Rongbiao Pi and Yumin Hu and Peng Huang and Shijun Wen",

note = "Funding Information: This work was supported in part by National Natural Science Foundation of China (81672952, 81430060), and Guangdong Science and Technology Program (2017A020215198). Publisher Copyright: {\textcopyright} 2018 The Royal Society of Chemistry.",

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T2 - N -arylsulfonyl carbazoles as novel anticancer agents

AU - You, Xin

AU - Zhu, Daqian

AU - Lu, Wenhua

AU - Sun, Yichen

AU - Qiao, Shuang

AU - Luo, Bingling

AU - Du, Yongliang

AU - Pi, Rongbiao

AU - Hu, Yumin

AU - Huang, Peng

AU - Wen, Shijun

N1 - Funding Information: This work was supported in part by National Natural Science Foundation of China (81672952, 81430060), and Guangdong Science and Technology Program (2017A020215198). Publisher Copyright: © 2018 The Royal Society of Chemistry.

PY - 2018

Y1 - 2018

N2 - 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.

AB - 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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Design, synthesis and biological evaluation of: N -arylsulfonyl carbazoles as novel anticancer agents

Abstract

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