- Synthesis and evaluation of the antitumor activity of polyhalo acridone derivatives
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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.
- Huang, Chao,Yan, Sheng-Jiao,Zeng, Xiang-Hui,Sun, Bo,Lan, Min-Bo,Lin, Jun
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p. 17444 - 17450
(2015/05/19)
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