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Synthesis, structure and in vitro cytotoxicity testing of some 2-aroylbenzofuran-3-ols.
Acta Crystallographica Section C ( IF 0.8 ) Pub Date : 2020-08-13 , DOI: 10.1107/s2053229620011018
Nguyen Tien Cong 1 , Huynh Thi Xuan Trang 1 , Pham Duc Dung 1 , Tran Hoang Phuong 2 , Vu Quoc Trung 3 , Nguyen Dang Dat 3 , Dang Thi Tuyet Anh 4 , Nguyen Van Tuyen 4 , Luc Van Meervelt 5
Affiliation  

Five 2‐aroyl‐5‐bromobenzo[b]furan‐3‐ol compounds (two of which are new) and four new 2‐aroyl‐5‐iodobenzo[b]furan‐3‐ol compounds were synthesized starting from salicylic acid. The compounds were characterized by mass spectrometry and 1H NMR and 13C NMR spectroscopy. Single‐crystal X‐ray diffraction studies of four compounds, namely, (5‐bromo‐3‐hydroxybenzofuran‐2‐yl)(4‐fluorophenyl)methanone, C15H8BrFO3, (5‐bromo‐3‐hydroxybenzofuran‐2‐yl)(4‐chlorophenyl)methanone, C15H8BrClO3, (5‐bromo‐3‐hydroxybenzofuran‐2‐yl)(4‐bromophenyl)methanone, C15H8Br2O3, and (4‐bromophenyl)(3‐hydroxy‐5‐iodobenzofuran‐2‐yl)methanone, C15H8BrIO3, were also carried out. The compounds were tested for their in vitro cytotoxicity on the four human cancer cell lines KB, Hep‐G2, Lu‐1 and MCF7. Six compounds show good inhibiting abilities on Hep‐G2 cells, with IC50 values of 1.39–8.03 µM.

中文翻译:

一些2-芳酰基苯并呋喃-3-醇的合成,结构和体外细胞毒性测试。

从水杨酸开始合成了5种2芳酰基5溴苯并[ b ]呋喃3-醇化合物(其中2种是新化合物)和4种新的2芳酰基5碘苯并[ b ]呋喃3-醇化合物。通过质谱,1 H NMR和13 C NMR光谱对化合物进行表征。四种化合物的单晶X射线衍射研究,即(5-溴-3-羟基苯并呋喃-2-基)(4-氟苯基)甲酮,C 15 H 8 BrFO 3,(5-溴-3-羟基苯并呋喃2-基)(4-氯苯基)甲酮,C 15 H 8 BrClO 3,(5-溴-3-基羟基苯并呋喃-2-基)(4-溴苯基)甲酮,C 15 H 8还进行了Br 2 O 3和(4-溴苯基)(3-羟基-5-碘苯并呋喃-2-基)甲酮C 15 H 8 BrIO 3的研究。测试了这些化合物对四种人类癌细胞系KB,Hep-G2,Lu-1和MCF7的体外细胞毒性。六种化合物对Hep‐G2细胞具有良好的抑制能力,IC 50值为1.39–8.03 µM
更新日期:2020-08-13
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