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Citation: Wen Qianwen, Li Yong, Su Zhengying, Wan Li. Design and Synthesis of 4-(5H-Pyrimido[5, 4-b]indol-2-yl-amino)Benzamide Derivatives as Antitumor Agents[J]. Chemistry, ;2019, 82(4): 350-358. shu

Design and Synthesis of 4-(5H-Pyrimido[5, 4-b]indol-2-yl-amino)Benzamide Derivatives as Antitumor Agents

Wen Qianwen ^1,2 ,
Li Yong ² ,
Su Zhengying ² ,
Wan Li ^1,,

1.
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137
2.
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041

Corresponding author: Wan Li, wanli8801@163.com
Received Date: 1 November 2018
Accepted Date: 10 December 2018

Figures(5)

Nineteen kinds of novel 4-(5H-pyrimido[5, 4-b]indol-2-yl-amino)benzamine derivatives were synthesized and evaluated for their in vitro antiproliferative activities. The structures of the as-synthesized compounds were confirmed by ¹H NMR, ¹³C NMR and HRMS. Their anti-tumor activity against HCT116, MD-MBA-231, C6, A549 and MCF-7 cancer cell lines were tested by MTT assay. All compounds showed good anti-tumor activity, especially compounds 5a, 5b, 5c, 5e, 5i, 5p and 5r showed 20 to 100 folds activity enhancement than the positive control 5-fluorouracil. The IC₅₀ values of 5b for tumor cells HCT116, MD-MBA-231, C6, A549 and MCF-7 were 3.26, 3.06, 0.63, 0.68, 2.32 μmol/L, respectively. Preliminary results indicated that these compounds have significant inhibitory effects on tumor cell proliferation and provide ideas for the design and synthesis of novel 5H-pyrimido[5, 4-b]indol-2-amine based antitumor compounds.
- 9 H-pyrimido[4, 5-b] indole,
- Benzamide,
- Synthesis,
- Anti-tumor activity
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