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Short Paper | Regular issue | Vol 89, No. 8, 2014, pp.1923-1932
Published online, 13th June, 2014
DOI: 10.3987/COM-14-13036
Design, Synthesis and Antiproliferative Activity Evaluation of New 5-Azaisoindigo Derivatives

Ping Zhao, Yun Yan, Yanzhong Li, Aiying Zhang, Xiaoping Zhan, Zenglu Liu, Zhenmin Mao,* Shaoxiong Chen, and Liqun Wang

*School of Pharmacy, Shanghai Jiaotong University , No.800 Dongchuan Road, Minhang District, Shanghai 200240, China


New 5-azaisoindigo derivatives were synthesized with two key intermediates 5-azaoxindole (7) and substituted indole-2,3-dione (10) in this paper. Intermediate 7 was prepared using 3-methylpridine (1) as the starting material via oxidation, nitration, condensation and cyclization, bromination and reduction reactions. Intermediate 10 was obtained by a convenient Sandmeyer’s method. The target compounds 5-azaisoindigo derivatives 11a-f were obtained by condensation of these two intermediates 7 and 10 in acidic condition. All target compounds were evaluated for their antiproliferative activity against seven cell lines by SRB assay. Compounds 11e and 11f showed significant antiproliferative activity against K562 cells (IC50: 8.9 µM and 13.6 µM, respectively).