102122-03-2Relevant academic research and scientific papers
Synthesis of polyhalo acridones as pH-sensitive fluorescence probes
Huang, Chao,Yan, Sheng-Jiao,Li, Yan-Mei,Huang, Rong,Lin, Jun
, p. 4665 - 4669 (2010)
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.
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.
