You Xin, Zhu Daqian, Lu Wenhua, Sun Yichen, Qiao Shuang, Luo Bingling, Du Yongliang, Pi Rongbiao, Hu Yumin, Huang Peng, Wen Shijun
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.
RSC Adv. 2018 May 10;8(31):17183-17190. doi: 10.1039/c8ra02939c. eCollection 2018 May 9.
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.
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。