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新型抗癌药物——芳基磺酰基咔唑的设计、合成及生物学评价

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

作者信息

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

机构信息

Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, Sun Yat-sen University 651 Dongfeng East Road Guangzhou 510060 China

School of Pharmaceutical Sciences, Sun Yat-sen University 132 Waihuan East Road Guangzhou 510006 China.

出版信息

RSC Adv. 2018 May 10;8(31):17183-17190. doi: 10.1039/c8ra02939c. eCollection 2018 May 9.

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 -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 study demonstrated that 8h prevented the tumor growth in PANC-1 and Capan-2 xenograft models without apparent toxicity.

摘要

在这项工作中,筛选了一组结构多样的合成咔唑类化合物的抗癌活性。根据构效关系研究,具有对位取代磺酰基的咔唑类化合物表现出更好的抗癌活性。此外,发现化合物8h通过诱导细胞凋亡和使细胞周期停滞在G2/M期,对Capan-2细胞显示出最有效的抗癌作用。最后,该研究表明8h可抑制PANC-1和Capan-2异种移植模型中的肿瘤生长,且无明显毒性。

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