Synthesis and anti-tumor activity<i> in vitro</i> of<i> N</i>-hetercycle substituted benzofuran derivatives

MAO Zewei; WAN Chunping; JIANG Yuan; GUO Wenlian; RAO Gaoxiong

doi:10.11665/j.issn.1000-5048.20150106

Journal of China Pharmaceutical University > 2015 > 46(1): 58-61. > DOI: 10.11665/j.issn.1000-5048.20150106

MAO Zewei, WAN Chunping, JIANG Yuan, GUO Wenlian, RAO Gaoxiong. Synthesis and anti-tumor activity in vitro of N-hetercycle substituted benzofuran derivatives[J]. Journal of China Pharmaceutical University, 2015, 46(1): 58-61. DOI: 10.11665/j.issn.1000-5048.20150106

Citation:

PDF (965 KB)

Synthesis and anti-tumor activity in vitro of N-hetercycle substituted benzofuran derivatives

More Information

Graphical Abstract

Abstract

Abstract

To discover the novel compounds with biological activity, N-hetercycle substituted derivatives were synthesized based on the structure of benzofuran. A series of novel N-hetercycle substituted benzofuran derivatives( 2a - 2j )were synthesized by the reaction of 2-(4′-florobenzoyl)benzofuran with N-heterocyclic compounds. And the structures were characterized by ¹H NMR, ¹³C NMR and HRMS. Their anti-tumor activities were studied in vitro against a panel of human tumor cell lines(HeLa, A549 and H1975)by the MTT assay. The results indicate that compounds 2a , 2f and 2j are the most potent within this series of compounds against human tumor cell lines, showing that they are promising lead compounds for further structural modifications and biological evaluation.
- N-hetercycle,
- benzofuran derivatives,
- synthesis,
- anti-tumor activity

FullText(HTML)

References (11)

References

[1]	Akgul YY,Anil H.Benzofurans and another constituent from seeds of Styrax officinalis[J].Phytochemistry,2003,63(8):939-943.
[2]	Sheen WS,Tsai IL,Teng CM,et al.Nor-neolignan and phenyl propanoid from Zanthoxylum ailanthoides[J].Phytochemistry,1994,36(1):213-215.
[3]	Pauletti PM,Araújo AR,Young MC,et al.Nor-lignans from the leaves of Styrax ferrugineus (Styracaceae)with antibacterial and antifungal activity[J].Phytochemistry,2000,55(6):597-601.
[4]	Pacher T,Seger C,Engelmeier D,et al.Antifungal stilbenoids from Stemona collinsae[J].J Nat Prod,2002,65(6):820-827.
[5]	Romeo R,Pier G,Taradas S,et al.Synthesis and biological evaluation of 2-( 3′,4′,5′-trimethoxybenzoyl)-3-N,N-dimethylaminobenzo[b]furan derivatives as inhibitors of tubulin polymerization[J].Bioorg Med Chem,2008,16(18):8419-8426.
[6]	Shen F,Hu AX,Luo XF,et al.Synthesis and bioactivity of(E)-2-benzylidenimino-4-(7-methoxy-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)thiazole[J].Chin J Org Chem(有机化学),2012,32(2):388-392.
[7]	Wang B,Lai YS,Zhang YH.Advances in the research of benzofuran compounds[J].Prog Pharm Sci(药学进展),2008,32(8):351-356.
[8]	Zhou JM,Ni PZ,Fu JH,et al.Synthesis and hypotensive activity of benzofuran and dihydrobenzofuran analogues[J].J China Pharm Univ(中国药科大学学报),1999,30(6):401-405.
[9]	Yang XD,Wan WC,Deng XY,et al.Design,synthesis and cytotoxic activities of novel hybrid compounds between 2-phenylbenzofuran and imidazole[J].Bioorg Med Chem Lett,2012,22(8):2726-2729.
[10]	Mao ZW,Guo WL,Jiang Y,et al.Synthesis of novel 2-benzoyl benzo[b]furan derivatives[J].Chin J Synth Chem(合成化学),2014,22(6):785-788.
[11]	Mao ZW,Wan CP,Zheng X,et al.Synthesis and biological activities of novel hybrid compounds between piperazine and acetophenone[J].J China Pharm Univ(中国药科大学学报),2014,45(5):517-521.

Cited By

Get Citation

PDF

XML

Article views (1460) PDF downloads (2063)

Turn off MathJax

Article Contents

Abstract

References

Synthesis and anti-tumor activity in vitro of N-hetercycle substituted benzofuran derivatives

Abstract

References

Catalog

Export File

Citation

Format

Content