104569-02-0Relevant academic research and scientific papers
Synthesis and evaluation of the antitumor activity of polyhalo acridone derivatives
Huang, Chao,Yan, Sheng-Jiao,Zeng, Xiang-Hui,Sun, Bo,Lan, Min-Bo,Lin, Jun
, p. 17444 - 17450 (2015/05/19)
A series of polyhalo acridone heterocyclic compounds were synthesized and evaluated for their in vitro antitumor activity. It was noteworthy that halogen atoms were present at the 1, 3 and 4 sites of the compounds, and an amide group or a cyano group was at the 2 site. The antitumor bioactivity screening revealed that all the compounds exhibited potent antitumor activity. In particular, compounds 4d, 4o, 5j and 5k showed good antineoplastic selectivity, with a survival rate above 50% in NIH3T3 mouse embryonic cells. The IC50 values were 8.69-13.06 μM in A431 cells. A preliminary assessment of the structure-selectivity relationship of the compounds was also performed.
Synthesis and antimicrobial activity of polyhalo isophthalonitrile derivatives
Huang, Chao,Yan, Sheng-Jiao,He, Neng-Qin,Tang, Ya-Juan,Wang, Xing-Hong,Lin, Jun
supporting information, p. 2399 - 2403 (2013/05/09)
A series of polyhalo isophthalonitrile derivatives (3 and 4) that incorporate a variety of substituents at the 2-, 4-, 5- and/or 6-positions of the isophthalonitrile moieties have been designed and synthesized. These derivatives were evaluated for their antimicrobial activity against Staphylococcus aureus, Bacillus cereus (Gram-positive bacteria), Escherichia coli, Pseudomonas aeruginosa (Gram-negative bacteria); and Candida albicans (Fungi). Compounds 3 and 4 showed stronger inhibition of Gram-positive bacteria and fungi growth, and the antimicrobial ability of compound 3j (a 4-(benzylamino)-5-chloro-2,6-difluoro analog, MIC[SA] = 0.5 μg/mL; MIC[BC] = 0.4 μg/mL; MIC[CA] = 0.5 μg/mL) were close to nofloxacin and fluconazole and identified as the most potent antimicrobial agents in the series. The preliminary analysis of structure-activity relationships is also discussed.
Synthesis of polyhalo acridones as pH-sensitive fluorescence probes
Huang, Chao,Yan, Sheng-Jiao,Li, Yan-Mei,Huang, Rong,Lin, Jun
supporting information; experimental part, p. 4665 - 4669 (2010/10/02)
Polyhalo isophthalonitriles were reacted with substituted anilines and subsequently cyclocondensed in the presence of sulfuric acid to give polyhalo acridones. These polyhalo acridones were proven to be useful as pH-sensitive fluorescent probes for a wide range of acidic and basic conditions.
