953798-17-9Relevant academic research and scientific papers
Synthesis of carbazole derivatives containing chalcone analogs as non-intercalative topoisomerase II catalytic inhibitors and apoptosis inducers
Li, Peng-Hui,Jiang, Hong,Zhang, Wen-Jin,Li, Yong-Lian,Zhao, Min-Cong,Zhou, Wei,Zhang, Lan-Yue,Tang, Ya-Dong,Dong, Chang-Zhi,Huang, Zhi-Shu,Chen, Hui-Xiong,Du, Zhi-Yun
, p. 498 - 510 (2018)
Novel topoisomerase II (Topo II) inhibitors have gained considerable interest for the development of anticancer agents. In this study, a series of carbazole derivatives containing chalcone analogs (CDCAs) were synthesized and investigated for their Topo II inhibition and cytotoxic activities. The results from Topo II mediated DNA relaxation assay showed that CDCAs could significantly inhibit the activity of Topo II, and the structure-activity relationship indicated the halogen substituent in phenyl ring play an important role in the activity. Further mechanism studies revealed that CDCAs function as non-intercalative Topo II catalytic inhibitors. Moreover, some CDCAs showed micromolar cytotoxic activities. The most potent compound 3h exhibited notable growth inhibition against four human cancer cell lines. Flow cytometric analysis revealed that compounds 3d and 3h arrested the HL-60 cells in sub G1 phase by induction of apoptosis. It was further confirmed by Annexin-V-FITC binding assay. Western blot analysis revealed that compound 3h induces apoptosis likely through the activation of caspase proteins.
Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors
Jiang, Hong,Zhang, Wen-Jin,Li, Peng-Hui,Wang, Jian,Dong, Chang-Zhi,Zhang, Kun,Chen, Hui-Xiong,Du, Zhi-Yun
, p. 1320 - 1323 (2018/03/21)
In this study, a series of carbazole-rhodanine conjugates was synthesized and evaluated for their Topoisomerase II inhibition potency as well as cytotoxicity against a panel of four human cancer cell lines. Among these thirteen compounds, 3a, 3b, 3g, and
CARBAZOLE COMPOUND
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Page/Page column 82, (2010/11/28)
The present invention provides a carbazole compound represented by formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R1 is a hydrogen atom, etc; R2 is a lower alkoxy group, etc; and R3 is a hydrogen atom, etc. The carbazole compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.
