14658-65-2Relevant academic research and scientific papers
Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors
Dong, Guoqiang,Fang, Yuxin,Liu, Yang,Liu, Na,Wu, Shanchao,Zhang, Wannian,Sheng, Chunquan
supporting information, p. 1929 - 1933 (2017/04/07)
Previously, 4-tosylanthra[1,2-c][1,2,5]thiadiazole-6,11-dione (1) was identified as a novel non-camptothecin topoisomerase I (Top1) inhibitor by structure-based virtual screening. Herein, a series of 4-substituted derivatives were designed and synthesized. Most of them showed potent Top1 inhibitory activity. Their in vitro antiproliferative activity was also evaluated in A549, HCT-116 and ZR-75-30 human cancer cell lines. Compound 8s showed good antiproliferative activity with IC50 of 0.52?μM and 0.42?μM against HCT-116 and ZR-75-30 cell line, respectively. Top1 unwinding assay and molecular modeling studies rationalized the mode of action of this new class of inhibitors.
4-substituted anthracene and [1,2-c] [1, 2, 5] thiadiazole -6,11-dione derivatives and its preparation method and application
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Paragraph 0154-0155, (2016/10/09)
The invention relates to the technical field of medicine. The invention provides a 4-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivative and its pharmaceutically acceptable salt. The structural general formula of the compound is as shown in
Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c[[1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents
Lee, Yu-Ru,Chen, Tsung-Chih,Lee, Chia-Chung,Chen, Chun-Liang,Ahmed Ali, Ahmed Atef,Tikhomirov, Alexander,Guh, Jih-Hwa,Yu, Dah-Shyong,Huang, Hsu-Shan
, p. 661 - 676 (2015/09/21)
A series of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-diones were synthesized and evaluated using the cell proliferations, apoptosis and NCI-60 cell panel assays. Also, the signaling pathways that account for their activities were investigated. Compounds 2, 3, 4a, 4d, 4f, 4i, 4k, 5b, 5c, 5d, 5f, 5g, 6b, 6c, 6d, 6e, 6g, 7a and 7g were selected by NCI. Among the tested compounds, 6g appeared to be the most active compound of this series that not only induced apoptosis in DU-145 cancer cells but also attenuated the ERK1/2 and p38 signaling pathways. All test compounds exhibited diverse cytostatic and cytotoxic activities that warrant further development as potential anticancer agents.
HETEROCYCLIC FUSED ANTHRAQUINONE DERIVATIVES, MANUFACTURING METHOD AND PHARMACEUTICAL COMPOSITION USING THEREOF
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Paragraph 0095 - 0100, (2013/11/06)
A heterocyclic fused anthraquinone derivatives, which is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of hydrogen, halogens, aminoalkyl group, sulfoalkyl group, haloalkyl group, piperazino
