98994-93-5Relevant academic research and scientific papers
The synthesis of furoquinolinedione and isoxazoloquinolinedione derivatives as selective Tyrosyl-DNA phosphodiesterase 2 (TDP2) inhibitors
Yang, Hao,Zhu, Xiao-Qing,Wang, Wenjie,Chen, Yu,Hu, Zhu,Zhang, Yu,Hu, De-Xuan,Yu, Le-Mao,Agama, Keli,Pommier, Yves,An, Lin-Kun
, (2021)
Based on our previous study on the development of the furoquinolinedione and isoxazoloquinolinedione TDP2 inhibitors, the further structure–activity relationship (SAR) was studied in this work. A series of furoquinolinedione and isoxazoloquinolinedione de
Transition metal complexes with 6,7-dichloro-5,8-quinolinedione as mitochondria-targeted anticancer agents
Huang, Xiao-Ling,Liang, Hong,Qin, Qi-Pin,Tan, Ming-Xiong,Wang, Zhen-Feng,Wu, Xue-Yu,Zou, Bi-Qun
, (2020/03/11)
Herein, a series of transition metal complexes, [Zn(DQ)2(CH3OH)2] (1), [Zn(DMQ)2(CH3OH)2] (2), [Co(DQ)2(CH3OH)2] (3), [Co(DMQ)2(CH3OH)2] (4), [Ni(DQ)2(CH3OH)2] (5), [Cu(DMQ)2(CH3OH)2] (6), [Mn(DQ)2(H2O)2] (7) and [Mn(DMQ)2(H2O)2] (8), containing 6,7-dichloro-5,8-quinolinedione (DQ) and 6,7-dichloro-2-methyl-5,8-quinolinedione (DMQ) ligands have been synthesized and characterized as potential antitumor agents. These complexes 1–8 exhibited evident anti-tumor activity in HeLa (cervical), MCF-7 (breast), Hep-G2 (hepatoma), T-24 (bladder), and SK-OV-3 (ovarian) human cancer cells. Interestingly, complexes 1–8 showed higher cytotoxicity than cisplatin against human cervical HeLa cells, and less cytotoxicity on the HL-7702 nontumorigenic cells. Mechanism studies suggested that complexes 1 and 2 arrested the cell cycle in the G1 phase and induced cancer cell death through mitochondrial dysfunction pathways. The cytotoxicity of 2 was higher than that of 1. The different biological behavior of 1 and 2 may correlate with the presence of a 2-methyl group in 6,7-dichloro-2-methyl-5,8-quinolinedione (DMQ) ligand. In general, our study demonstrated that Zn(II) complex 2 with 6,7-dichloro- 2-methyl-5,8-quinolinedione showed high potential to be developed as a mitochondria-targeted metal antitumor agent.
The synthesis and evaluation of quinolinequinones as anti-mycobacterial agents
Santoso, Kristiana T.,Menorca, Ayana,Cheung, Chen-Yi,Cook, Gregory M.,Stocker, Bridget L.,Timmer, Mattie S.M.
, p. 3532 - 3545 (2019/07/03)
A library of thirty-two quinolinequinones (QQs) with various amine substituents at the 6- and 7-positions were synthesised efficiently and in good yields for evaluation as potential anti-tuberculosis agents. Mycobacterium tuberculosis growth inhibition as
The anti-cancer, anti-inflammatory and tuberculostatic activities of a series of 6,7-substituted-5,8-quinolinequinones
Mulchin, Benjamin J.,Newton, Christopher G.,Baty, James W.,Grasso, Carole H.,Martin, William John,Walton, Michaela C.,Dangerfield, Emma M.,Plunkett, Catherine H.,Berridge, Michael V.,Harper, Jacquie L.,Timmer, Mattie S.M.,Stocker, Bridget L.
experimental part, p. 3238 - 3251 (2010/07/08)
A variety of 6,7-substituted-5,8-quinolinequinones were synthesised and assessed for their anti-tumour and anti-inflammatory activities, and their ability to inhibit the growth of Mycobacterium bovis BCG. In particular, the introduction of a sulfur group
