1744-91-8Relevant articles and documents
3-Nitroacridine derivatives arrest cell cycle at G0/G1 phase and induce apoptosis in human breast cancer cells may act as DNA-target anticancer agents
Zhou, Qian,You, Chaoqun,Zheng, Cong,Gu, Yawen,Gu, Hongchao,Zhang, Rui,Wu, Hongshuai,Sun, Baiwang
, p. 1 - 9 (2018)
DNA is considered to be one of the most promising targets for anticancer agents. Acridine analogues have anticancer activity based on DNA binding and topoisomerases inhibition. However, due to the side effects, resistance and low bioavailability, a few have entered into clinical usage and the mechanisms of action are not fully understood. Novel acridine derivatives are needed for effective cancer therapy. A series of novel 3-nitroacridine-based derivatives were synthesized, their DNA binding and anticancer activities were evaluated. The chemical modifications at position 9 of the 3-nitroacridine were crucial for DNA affinity, thus optimizing anticancer activity. UV–Vis and circular dichroism (CD) spectroscopy indicated interaction of compounds with DNA, and the binding modes were intercalation and groove binding. MTT assay and clonogenic assay showed that compounds 1, 2 and 3 had obvious cell growth inhibition effect. They induced cell apoptosis in human breast cancer cells in a dose-dependent manner, and exhibited anticancer effect via DNA damage as well as cell cycle arrest at G0/G1 phage. Using confocal fluorescent microscope, the apoptotic features were observed. The results suggested that compounds 1–3 with high DNA binding affinity and good inhibitory effect of cancer cell proliferation can be developed as prime candidates for further chemical optimization.
Identification of novel 3-nitroacridines as autophagy inducers in gastric cancer cells
Yu, Jia,Zhao, Xiaoqing,Zhang, Nanmengzi,You, Chaoqun,Yao, Gang,Zhu, Jin,Xu, Liang,Sun, Baiwang
, p. 4087 - 4095 (2017/07/12)
Dysregulated autophagy is involved in various human disorders including cancer. An autophagy-associated cell death pathway can be seen as a back-up cell death mechanism in cancer cells that are deficient in the apoptosis pathway. Therefore, many attempts have been made to induce autophagy for anticancer therapy. Anti-apoptotic Bcl-2 family proteins Bcl-2 and Bcl-xL can inhibit autophagy via binding to the BH3-only protein Beclin 1, an essential autophagy stimulator. In a previous study, we discovered several small molecule Beclin 1 mimetics as autophagy inducers through high-throughput screening and structural optimization, in which 3-nitroacridine warrants further exploration. Here, a series of novel 3-nitroacridine derivatives were designed, synthesized, and their pharmaceutical activities and mechanism of action were investigated against gastric cancer cell lines. As a result, compounds 3, 4, and 9 displayed potent cytotoxicity and induced autophagy in MGC-803 and SGC-7901 gastric cancer cells. Besides, compounds 3 and 9 also inhibited the migration of SGC-7901 cells. The development of 3-nitroacridine analogues as autophagy inducers is not only likely to be a potential strategy for cancer therapy, but it will also facilitate a better understanding of the complicated roles of autophagy in normal physiology and pathophysiology.
NOVEL FLUORESCENT DYES AND USES THEREOF
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, (2014/04/04)
The present invention relates to fluorescent dyes based on acridine derivatives and use of such dyes, for example, in biochemical and/or cell based assays. A preferred feature of some of the dyes described is their long fluorescence lifetimes and their us
