Furanylazaindoles: Potent anticancer agents in vitro and in vivo

Hsueh Yun Lee, Shiow Lin Pan, Min-Chieh Su, Yi-Min Liu, Ching-Chuan Kuo, Yi-Ting Chang, Jian-Sung Wu, Chih-Ying Nien, Samir Mehndiratta, Chi-Yen Chang, Su-Ying Wu, Mei-Jung Lai, Jang-Yang Chang, Jing Ping Liou

研究成果: 雜誌貢獻文章同行評審

47 引文 斯高帕斯(Scopus)


Preliminary biological data on 7-anilino-6-azaindoles (8-11) suggested that hydrophobic substituents at C7 contribute to enhancement of antiproliferative activity. A novel series of 7-aryl-6-azaindole-1-benzenesulfonamides (12-22) were developed and showed improved cytotoxicity compared to ABT751 (5). The conversion of C7 phenyl rings into C7 heterocycles led to a remarkable improvement of antiproliferative activity. Among all the synthetic products, 7-(2-furanyl)-1-(4-methoxybenzenesulfonyl)-6-azaindole (21) exhibited the most potent anticancer activity against KB, HT29, MKN45, and H460 cancer cell lines with IC50 values of 21.1, 32.0, 27.5, and 40.0 nM, respectively. Bioassays indicated that 21 not only inhibits tubulin polymerization by binding to tubulin at the colchicine binding site but also arrests the cell cycle at the G2/M phase with slight arrest at the sub-G1 phase. Compound 21 also functions as a vascular disrupting agent and dose-dependently inhibits tumor growth without significant change of body weight in an HT29 xenograft mouse model. Taken together, compound 21 has potential for further development as a novel class of anticancer agents.
頁(從 - 到)8008-8018
期刊Journal of Medicinal Chemistry
出版狀態已發佈 - 10月 24 2013

ASJC Scopus subject areas

  • 分子醫學
  • 藥物發現


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