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Molecules 2016, 21(4), 516; doi:10.3390/molecules21040516

Synthesis and Antitumor Evaluation of Novel 5-Hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one Derivatives

1
Individualized Medication Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People’s Hospital, Chinese Academy of Sciences Sichuan Translational Medicine Research Hospital, School of Medicine, Center for Information in Medicine, University of Electronic Science and Technology of China, Chengdu 610072, Sichuan, China
2
Bioengineering College, Xihua University, Chengdu 610039, Sichuan, China
3
State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 26 January 2016 / Revised: 21 March 2016 / Accepted: 31 March 2016 / Published: 20 April 2016
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Abstract

A series of novel 5-hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one derivatives bearing natural product substructures has been successfully synthesized and their antitumor activity studied. These newly synthesized derivatives were characterized by 1H-NMR, 13C-NMR and high resolution mass spectral data, then screened as antitumor agents against the A549, HCC1937, and MDA-MB-468 human tumor cell lines using MTT cell proliferation assays. The results show that some of these compounds can effectively inhibit the growth of these cancerous cells, with compound 5b being the best one (IC50 = 2.6 μM). Flow cytometry data revealed that compound 5b induced apoptosis of HCC1937 cells with increased solution concentration. The structure and activity relationships (SAR) of these compounds is summarized. View Full-Text
Keywords: antitumor activity; 5-hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one; synthesis antitumor activity; 5-hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one; synthesis
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Ouyang, G.; Tong, R.; Li, J.; Bai, L.; Ouyang, L.; Duan, X.; Li, F.; He, P.; Shi, J.; He, Y. Synthesis and Antitumor Evaluation of Novel 5-Hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one Derivatives. Molecules 2016, 21, 516.

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